Category: 105628-07-7

Determination of homopiperazine in fasudil hydrochloride injection by UPLC-MS/MS was written by Shao, Hong-xia;Wang, Hui;Qin, Qiu-ming. And the article was included in Zhejiang Huagong in 2021.Application In Synthesis of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

Objective: To establish an ultra high performance liquid phase-tandem mass spectrometry (UPLC-MS/MS) method for the determination of homopiperazine in fasudil hydrochloride injection. Methods: The sample was diluted with an appropriate amount of 1 mol·L^-1 sodium hydroxide solution, then extracted and injected with acetonitrile. The optimal conditions were mobile phase: methanol-0.1% formic acid aqueous solution, column: Acquity UPLC BEH C18 (2.1 mm × 100 mm, 1.7 μm). Multiple reaction monitoring (MRM) mode was performed with Electron Spray Ionization (ESI) operating in the pos. ionization mode. Results: Homopiperazine had a good linear relationship within 360-2400 μg·L^-1 (correlation coefficient r = 0.9977). The relative average deviation (RSD) of the repeatability tests was 1%, the recovery rate was 87-100%, and the LOD (S/N was about 3) was 60 μg·L^-1. The sample solution was stable within 24 h at room temperature Conclusion: This experiment has established a method for the determination of homopiperazine in fasudil hydrochloride injection. This method has the advantages of simple pretreatment, rapid anal., high sensitivity, accurate determination results, and strong specificity, and can be applied to the quality monitoring of drugs. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Application In Synthesis of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Quinoline and its derivatives are widely used as fungicides, biological agents, antibiotics, alkaloids, dyes, rubber chemicals and flavoring agents. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Application In Synthesis of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Effect of hydrochloride fasudil on serum TGF-β₁ and MCP-1 in early diabetic nephrosis patients was written by Huang, Cong. And the article was included in Biaoji Mianyi Fenxi Yu Linchuang in 2015.Recommanded Product: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

Objective To explore the changes of serum TGF-β₁ and MCP-1 in diabetic nephrosis patients after treated with Fasudil injection. Methods 100 early diabetic nephrosis patients were randomly divided into the group A (control group,50 cases) and group B(50 cases). AU patients received routine therapy, while patients in group B were addnl. given fasudil injection for 2 wk. The level of serum TGF-β₁ and MCP-1 were measured by the ELISA before and after the treatment. Results After the treatment, the levels of TGF-β₁ and MCP-1 in group A had not significant Changes(P>0.05), While the levels of TGF-β₁ and MCP-1 in group B after treatment were much lower than that of before treatment(P <0.05). The decrease of TGF-β₁ and MCP-1 were more significant in group B than that of in group A after treatment( P < 0.05). Conclusion On the basis of routine therapy, Fasudil injection could inhibit the expression of TGF-β₁ and MCP-1, which has good curative effect on early diabetic nephrosis. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Recommanded Product: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Quinoline and isoquinoline skeletons are among the most attractive frameworks with a wide range of biological and pharmacological activities. Isoquinoline-type alkaloids show biological activities similar to those of morphinane-, protoberberine-, and benzophenanthridine-type alkaloids.Recommanded Product: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Effect of fasudil hydrochloride on the level of serum lysophosphatidic acid was written by Bi, Yu-hua;Zou, Li;Li, Xia. And the article was included in Linchuang Yixue in 2013.Reference of 105628-07-7 This article mentions the following:

To investigate the effect of fasudil hydrochloride on the level of serum lysophosphatidic acid (LPA) in patients with acute anterior circulation infarction, a total of 47 patients with acute anterior circulation infarction were randomly divided into fasudil group (n=23) and routine treatment group(n=24). Patients in routine treatment group were given routine treatment, and patients in fasudil group were given fasudil hydrochloride 30 mg, i.v. drip, twice a day for 14 days on the basis of traditional treatment. 4 ML of venous blood samples was taken to measure the levels of LPA before and after treatment. Results showed that the LPA levels in both groups were decreased after 14 days of treatment (P<0.05). However, the indicator in the fasudil group were improved more significantly compared with the routine treatment group (P<0.05). In summary, fasudil could decrease the levels of serum LPA and improve patient’s prognosis. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Reference of 105628-07-7).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Being an analog of pyridine, isoquinoline is a weak base, with a pKa of 5.14. They are also used to make oil-soluble dyes, food colorants, pharmaceuticals, pH indicators and other organic compounds. Reference of 105628-07-7

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Determination of residual solvents in fasudil hydrochloride by headspace gas chromatography was written by Ding, Quan. And the article was included in Fujian Fenxi Ceshi in 2011.Quality Control of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

A method for determination of ethanol, Et acetate in fasudil hydrochloride by headspace gas chromatog. on DB-624 column with FID detector was developed. Three residual solvents were completely separated The degree of separation was 19.0 for methanol and aether, 20.8 for aether and dichloromethane. Good linearity was achieved (r = 0.9993 for methanol, r = 0.9997 for aether, and r = 0.9963 for dichloromethane). The average recovery was 95.81% for ethanol, 93.11% for aether, and 92.85 for dichloromethane. The RSD of repetition was 1.8 for methanol, 3.4% for aether and 5.4% for dichloromethane. The detection limits was 0.08 μg/mL for methanol, 0.0007 μg/mL for aether, and 0.07 μg/mL for dichloromethane. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Quality Control of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. The isoquinoline structure occurs in a considerable number of alkaloids in widely separated plant families. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Quality Control of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Mechanism of fasudil hydrochloride postconditioning in protecting rats against myocardial ischemia/reperfusion injury was written by Jiang, Zhi-hui;Feng, Guang-zhi;Qian, Zhi-yong;Xu, Shu-dong. And the article was included in Zhonghua Laonian Xin Nao Xueguanbing Zazhi in 2013.COA of Formula: C14H18ClN3O2S This article mentions the following:

The mechanism of fasudil hydrochloride postconditioning in protecting rats against myocardial ischemia/reperfusion (I/R) injury was studied. Thirty SD rats were randomly divided into sham operation group, I/R group, ischemic postconditioning group, fasudil hydrochloride group and fasudil hydrochloride + YZ94002 group (6 in each group). The rats were sacrificed 180 min after reperfusion. Expressions of Bcl-2, Bax, caspase 3, Akt and P-Akt in myocardial tissue were detected by Western blot. The Bcl-2 expression level was significantly higher whereas the Bax and caspase 3 expression levels were significantly lower in ischemic postconditioning group and fasudil hydrochloride group than in I/R group (P<0.05). The Bcl-2 expression level was significantly lower whereas the Bax and caspase 3 expression levels were significantly higher in fasudil hydrochloride + LY294002 group than in fasudil hydrochloride group (P<0.05). The Akt expression level was significantly higher in fasudil hydrochloride group than in I/R group and fasudil hydrochloride+LYZ94002 group (P<0.05). Fasudil hydrochloride postconditioning can protect rats against myocardial I/R injury possibly by activating the PI3K-Akt pathway. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7COA of Formula: C14H18ClN3O2S).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Isoquinoline is a structural isomer of quinoline, which have antiseptic, antipyretic and anti-cyclic properties, and can be used as antimalarial drugs and for the preparation of other antimalarial medicine. They are also used to make oil-soluble dyes, food colorants, pharmaceuticals, pH indicators and other organic compounds. COA of Formula: C14H18ClN3O2S

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Determination of homopiperazine in fasudil hydrochloride injection by UPLC-MS/MS was written by Shao, Hong-xia;Wang, Hui;Qin, Qiu-ming. And the article was included in Zhejiang Huagong in 2021.Application In Synthesis of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

Objective: To establish an ultra high performance liquid phase-tandem mass spectrometry (UPLC-MS/MS) method for the determination of homopiperazine in fasudil hydrochloride injection. Methods: The sample was diluted with an appropriate amount of 1 mol·L^-1 sodium hydroxide solution, then extracted and injected with acetonitrile. The optimal conditions were mobile phase: methanol-0.1% formic acid aqueous solution, column: Acquity UPLC BEH C18 (2.1 mm × 100 mm, 1.7 μm). Multiple reaction monitoring (MRM) mode was performed with Electron Spray Ionization (ESI) operating in the pos. ionization mode. Results: Homopiperazine had a good linear relationship within 360-2400 μg·L^-1 (correlation coefficient r = 0.9977). The relative average deviation (RSD) of the repeatability tests was 1%, the recovery rate was 87-100%, and the LOD (S/N was about 3) was 60 μg·L^-1. The sample solution was stable within 24 h at room temperature Conclusion: This experiment has established a method for the determination of homopiperazine in fasudil hydrochloride injection. This method has the advantages of simple pretreatment, rapid anal., high sensitivity, accurate determination results, and strong specificity, and can be applied to the quality monitoring of drugs. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Application In Synthesis of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Quinoline and its derivatives are widely used as fungicides, biological agents, antibiotics, alkaloids, dyes, rubber chemicals and flavoring agents. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Application In Synthesis of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Effect of hydrochloride fasudil on serum TGF-β₁ and MCP-1 in early diabetic nephrosis patients was written by Huang, Cong. And the article was included in Biaoji Mianyi Fenxi Yu Linchuang in 2015.Recommanded Product: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

Objective To explore the changes of serum TGF-β₁ and MCP-1 in diabetic nephrosis patients after treated with Fasudil injection. Methods 100 early diabetic nephrosis patients were randomly divided into the group A (control group,50 cases) and group B(50 cases). AU patients received routine therapy, while patients in group B were addnl. given fasudil injection for 2 wk. The level of serum TGF-β₁ and MCP-1 were measured by the ELISA before and after the treatment. Results After the treatment, the levels of TGF-β₁ and MCP-1 in group A had not significant Changes(P>0.05), While the levels of TGF-β₁ and MCP-1 in group B after treatment were much lower than that of before treatment(P <0.05). The decrease of TGF-β₁ and MCP-1 were more significant in group B than that of in group A after treatment( P < 0.05). Conclusion On the basis of routine therapy, Fasudil injection could inhibit the expression of TGF-β₁ and MCP-1, which has good curative effect on early diabetic nephrosis. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Recommanded Product: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Quinoline and isoquinoline skeletons are among the most attractive frameworks with a wide range of biological and pharmacological activities. Isoquinoline-type alkaloids show biological activities similar to those of morphinane-, protoberberine-, and benzophenanthridine-type alkaloids.Recommanded Product: 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Effect of fasudil hydrochloride on the level of serum lysophosphatidic acid was written by Bi, Yu-hua;Zou, Li;Li, Xia. And the article was included in Linchuang Yixue in 2013.Reference of 105628-07-7 This article mentions the following:

To investigate the effect of fasudil hydrochloride on the level of serum lysophosphatidic acid (LPA) in patients with acute anterior circulation infarction, a total of 47 patients with acute anterior circulation infarction were randomly divided into fasudil group (n=23) and routine treatment group(n=24). Patients in routine treatment group were given routine treatment, and patients in fasudil group were given fasudil hydrochloride 30 mg, i.v. drip, twice a day for 14 days on the basis of traditional treatment. 4 ML of venous blood samples was taken to measure the levels of LPA before and after treatment. Results showed that the LPA levels in both groups were decreased after 14 days of treatment (P<0.05). However, the indicator in the fasudil group were improved more significantly compared with the routine treatment group (P<0.05). In summary, fasudil could decrease the levels of serum LPA and improve patient’s prognosis. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Reference of 105628-07-7).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Being an analog of pyridine, isoquinoline is a weak base, with a pKa of 5.14. They are also used to make oil-soluble dyes, food colorants, pharmaceuticals, pH indicators and other organic compounds. Reference of 105628-07-7

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Determination of residual solvents in fasudil hydrochloride by headspace gas chromatography was written by Ding, Quan. And the article was included in Fujian Fenxi Ceshi in 2011.Quality Control of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride This article mentions the following:

A method for determination of ethanol, Et acetate in fasudil hydrochloride by headspace gas chromatog. on DB-624 column with FID detector was developed. Three residual solvents were completely separated The degree of separation was 19.0 for methanol and aether, 20.8 for aether and dichloromethane. Good linearity was achieved (r = 0.9993 for methanol, r = 0.9997 for aether, and r = 0.9963 for dichloromethane). The average recovery was 95.81% for ethanol, 93.11% for aether, and 92.85 for dichloromethane. The RSD of repetition was 1.8 for methanol, 3.4% for aether and 5.4% for dichloromethane. The detection limits was 0.08 μg/mL for methanol, 0.0007 μg/mL for aether, and 0.07 μg/mL for dichloromethane. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Quality Control of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. The isoquinoline structure occurs in a considerable number of alkaloids in widely separated plant families. The Pomeranz–Fritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Quality Control of 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Design, synthesis and biological evaluations of a long-acting, hypoxia-activated prodrug of fasudil, a ROCK inhibitor, to reduce its systemic side-effects was written by Al-Hilal, Taslim A.;Hossain, Mohammad Anwar;Alobaida, Ahmad;Alam, Farzana;Keshavarz, Ali;Nozik-Grayck, Eva;Stenmark, Kurt R.;German, Nadezhda A.;Ahsan, Fakhrul. And the article was included in Journal of Controlled Release in 2021.Electric Literature of C14H18ClN3O2S This article mentions the following:

ROCK, one of the downstream regulators of Rho, controls actomyosin cytoskeleton organization, stress fiber formation, smooth muscle contraction, and cell migration. ROCK plays an important role in the pathologies of cerebral and coronary vasospasm, hypertension, cancer, and arteriosclerosis. Pharmacol.-induced systemic inhibition of ROCK affects both the pathol. and physiol. functions of Rho-kinase, resulting in hypotension, increased heart rate, decreased lymphocyte count, and eventually cardiovascular collapse. To overcome the adverse effects of systemic ROCK inhibition, we developed a bioreductive prodrug of a ROCK inhibitor, fasudil, that functions selectively under hypoxic conditions. By masking fasudil鈥瞫 active site with a bioreductive 4-nitrobenzyl group, we synthesized a prodrug of fasudil that is inactive in normoxia. Reduction of the protecting group initiated by hypoxia reveals an electron-donating substituent that leads to fragmentation of the parent mol. Under normoxia the fasudil prodrug displayed significantly reduced activity against ROCK compared to its parent compound, but under severe hypoxia the prodrug was highly effective in suppressing ROCK activity. Under hypoxia the prodrug elicited an antiproliferative effect on disease-afflicted pulmonary arterial smooth muscle cells and pulmonary arterial endothelial cells. The prodrug displayed a long plasma half-life, remained inactive in the blood, and produced no drop in systemic blood pressure when compared with fasudil-treated controls. Due to its selective nature, our hypoxia-activated fasudil prodrug could be used to treat diseases where tissue-hypoxia or hypoxic cells are the pathol. basis of the disease. In the experiment, the researchers used many compounds, for example, 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7Electric Literature of C14H18ClN3O2S).

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride (cas: 105628-07-7) belongs to isoquinoline derivatives. Although isoquinoline derivatives can be synthesized by several methods, relatively few direct methods deliver the unsubstituted isoquinoline. The Pomeranz鈥揊ritsch reaction provides a method for the preparation of isoquinoline. This reaction uses a benzaldehyde and aminoacetoaldehyde diethyl acetal, which in an acid medium react to form isoquinoline.Electric Literature of C14H18ClN3O2S

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem