Category: 156478-71-6

Inooka, Hiroshi; Sakamoto, Kotaro; Shinohara, Tokuyuki; Masuda, Yasushi; Terada, Michiko; Kumano, Satoshi; Yokoyama, Kotaro; Noguchi, Jiro; Nishizawa, Naoki; Kamiguchi, Hidenori; Fujita, Hisashi; Asami, Taiji; Takekawa, Shiro; Ohtaki, Tetsuya published an article about the compound: 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid( cas:156478-71-6,SMILESS:O=C(O)CN1CCN(C(OC(C)(C)C)=O)CC1 ).Related Products of 156478-71-6. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:156478-71-6) through the article.

Neuromedin U (NMU) is a neuropeptide known to regulate food intake and energy homeostasis that is widely distributed in the gastrointestinal tract, hypothalamus, and pituitary. A short form of NMU, porcine NMU-8 has potent agonist activity for the receptors NMUR1 and NMUR2; however, its short half-life precludes its effective use in vivo. To address this limitation, we designed and synthesized NMU-8 analogs modified by polyethylene glycol (PEG) with a mol. weight of 30 kDa (PEG30k) via a variety of linkers (i.e., ω-amino- and ω-imino-carboxylic acid linker). Integrated evaluation of NMUR1 and NMUR2 binding affinities in vitro and anorectic activity in mice revealed that the introduction of a linker with a rigid ring group, e.g., 2-(piperazin-1-yl)acetic acid (PipAc), yielded a highly potent anorectic peptide, PEG30k-PipAc-NMU-8 (14), possessing improved receptor binding affinity. Subsequent optimization of the mol. weight of the PEG moiety led to the discovery of a PEG20k conjugate (15), which exhibited significant anti-obesity effect upon once-daily s.c. administration in diet-induced obese mice with 10% and 22% body weight loss at doses of 10 and 30 nmol/kg, resp. In addition, 15 reduced the weights of the liver and adipose tissue in a dose-dependent manner and improved the plasma biochem. parameters, e.g., insulin, glutamic pyruvic transaminase, glutamic oxaloacetic transaminase, and total cholesterol. Thus, our results suggest that 15 (NMU-0002), which showed potent and long-lasting biol. profiles in vivo, represents a candidate peptide for investigating the central and peripheral actions of NMU and its potential for clin. use.

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Reference:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Henry, Sean; Anand, Jessica P.; Brinkel, Ashley C.; McMillan, Douglas M.; Twarozynski, Jack. J.; Loo, Christian E.; Traynor, John R.; Mosberg, Henry I. researched the compound: 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid( cas:156478-71-6 ).Synthetic Route of C11H20N2O4.They published the article 《SAR Matrices Enable Discovery of Mixed Efficacy μ-Opioid Receptor Agonist Peptidomimetics with Simplified Structures through an Aromatic-Amine Pharmacophore》 about this compound( cas:156478-71-6 ) in ACS Chemical Neuroscience. Keywords: opioid receptors peptidomimetics pharmacophore bifunctional ligands; bifunctional ligands; peptidomimetics; structure−activity relationship; δ-opioid receptor; κ-opioid receptor; μ-Opioid receptor. We’ll tell you more about this compound (cas:156478-71-6).

We previously described the development of potent μ-opioid receptor (MOR)-agonist/δ-opioid receptor (DOR)-antagonist peptidomimetic ligands as an approach toward effective analgesics with reduced side effects. In this series, a tetrahydroquinoline (THQ) or substituted Ph is employed to link two key pharmacophore elements, a dimethyltyrosine amino acid and typically an aromatic pendant. Using new and previously reported analogs, we constructed a structure-activity relationship (SAR) matrix that probes the utility of previously reported amine pendants. This matrix reveals that the MOR-agonist/DOR-antagonist properties of these ligands do not change when a tetrahydroisoquinoline (THIQ) pendant is used, despite removal of substituents on the core Ph ring. Based on this observation, we retained the THIQ pendant and replaced the Ph core with simpler aliphatic chain structures. These simpler analogs proved to be potent MOR-agonists with high variability in their effects at the DOR and the κ-opioid receptor (KOR). These data show that the amine of the THIQ pendant may be a novel pharmacophore element that favors high MOR-efficacy, whereas the aromatic ring of the THIQ pendant may produce high MOR-potency. Combined, the two pharmacophores within the THIQ pendant may be a structurally efficient means of converting opioid peptides and peptidomimetics into potent and efficacious MOR-agonists.

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Isoquinoline – Wikipedia,
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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications, published in 2020-10-22, which mentions a compound: 156478-71-6, mainly applied to PROTAC metabolism human hepatocytes ligands linkers CYP3A4 hAOX, Safety of 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid.

Hetero-bifunctional PROteolysis TArgeting Chimeras (PROTACs) represent a new emerging class of small mols. designed to induce polyubiquitylation and proteasomal-dependent degradation of a target protein. Despite the increasing number of publications about the synthesis, biol. evaluation, and mechanism of action of PROTACs, the characterization of the pharmacokinetic properties of this class of compounds is still minimal. Here, we report a study on the metabolism of a series of 40 PROTACs in cryopreserved human hepatocytes at multiple time points. Our results indicated that the metabolism of PROTACs could not be predicted from that of their constituent ligands. Their linkers’ chem. nature and length resulted in playing a major role in the PROTACs’ liability. A subset of compounds was also tested for metabolism by human cytochrome P 450 3A4 (CYP3A4) and human aldehyde oxidase (hAOX) for more in-depth data interpretation, and both enzymes resulted in active PROTAC metabolism

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Isoquinoline – Wikipedia,
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Reference of 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid, is researched, Molecular C11H20N2O4, CAS is 156478-71-6, about Synthesis and Pharmacological Evaluation of Tetrahydro-γ-carboline Derivatives as Potent Anti-inflammatory Agents Targeting Cyclic GMP-AMP Synthase. Author is Tan, Jing; Wu, Bing; Chen, Tingting; Fan, Chen; Zhao, Jiannan; Xiong, Chaodong; Feng, Chunlan; Xiao, Ruoxuan; Ding, Chunyong; Tang, Wei; Zhang, Ao.

The activation of cyclic GMP-AMP synthase (cGAS) by double-stranded DNA is implicated in the pathogenesis of many hyper inflammatory and autoimmune diseases, and the cGAS-targeting small mol. has emerged as a novel therapeutic strategy for treating these diseases. However, the currently reported cGAS inhibitors are far beyond maturity, barely demonstrating in vivo efficacy. Inspired by the structural novelty of compound I (G140), a structural optimization on both its side chain and the central tricyclic core, leads to several subseries of compounds, including those unexpectedly cyclized complex ones. Compound II (R = aminomethyl) bearing an N-glycylglycinoyl side chain was identified as the most potent one with cellular IC50 values of 1.38 and 11.4μM for h- and m-cGAS, resp. Mechanistic studies confirmed its direct targeting of cGAS. Further, compound II (R = aminomethyl) showed superior in vivo anti-inflammatory effects in the lipopolysaccharide-induced mouse model. The encouraging result of compound II (R = aminomethyl) provides solid evidence for further pursuit of cGAS-targeting inhibitors as a new anti-inflammatory treatment.

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Reference:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

SDS of cas: 156478-71-6. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid, is researched, Molecular C11H20N2O4, CAS is 156478-71-6, about Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.

Neuromedin U (NMU) is a neuropeptide that mediates a variety of physiol. functions via its receptors, NMUR1 and NMUR2. Recently, there has been an increased focus on NMU as a promising treatment option for diabetes and obesity. A short form of NMU (NMU-8) has potent agonist activity for both receptors but is metabolically unstable. Therefore, we designed and synthesized NMU-8 analogs modified by polyethylene glycol (PEG; mol. weight, 20 kDa; PEG20k) via a linker. 3-(2-Naphthyl)alanine substitution at position 19 increased NMUR2 selectivity of NMU-8 analogs with retention of high agonist activity. Compound 37, an NMUR2-selective PEG20k analog containing piperazin-1-ylacetyl linker, exhibited a potent body weight-lowering effect with concomitant inhibition of food intake in a dose-dependent manner (body weight loss of 12.4% at 30 nmol/kg) by once-daily repeated dosing for 2 wk in mice with diet-induced obesity.

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Quality Control of 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 2-(4-(tert-Butoxycarbonyl)piperazin-1-yl)acetic acid, is researched, Molecular C11H20N2O4, CAS is 156478-71-6, about A combinatorial approach to new DNA minor groove binders. Author is Behrens, Carsten; Nielsen, Peter E..

A combinatorial approach towards new DNA minor groove binders capable of recognizing GC base pairs is reported. From a partly AT-biased library of 5832 different octapeptides of the type Py-Py-X1-X2-X3-Py-Py-γAbu synthesized following the one bead one compound methodol., two compounds containing the central peptide sequences Val-βAla-Tyr and Pip-βAla-Tyr were selected by a fluorescence-double stranded DNA probing assay using the sequence 5′-TTTGTTT-3′ as the probe. The two hits were independently synthesized and binding to a recombinant pUC-19 EcoRl/Pvull DNA restriction fragment containing the sequence 5′-TTTGTTT-3′ demonstrated. Binding constants to eight targets in the DNA fragment were estimated from quant. DNAse I footprinting.

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Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem