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Submit ReviewSR 49059
说明： Selective, orally active vasopressin V1A receptor antagonist
别名： Relcovaptan
化学名： (2S)-1-[[(2R,3S)-5-Chloro-3-(2-chlorophenyl)-1-[(3,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-hydroxy-1H-indol-2-yl]carbonyl]-2-pyrrolidinecarboxamide
纯度： ≥99% (HPLC)
生物活性 for SR 49059
SR 49059 is a potent and selective non-peptide vasopressin V1A receptor antagonist; devoid of agonist activity. Displays high affinity and efficacy at both rat (Ki = 1.6 nM) and human (Ki = 1.1 - 6.3 nM) V1A receptors. Potently antagonizes arginine vasopressin-induced effects in vitro (IC50 = 3.7 nM for inhibition of human platelet aggregation) and is orally active in vivo.
化合物库 for SR 49059
SR 49059 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for SR 49059
| 分子量 | 620.5 |
| 公式 | C28H27Cl2N3O7S |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 150375-75-0 |
| PubChem ID | 60943 |
| InChI Key | CEBYCSRFKCEUSW-NAYZPBBASA-N |
| Smiles | O=S(C1=CC(OC)=C(OC)C=C1)(N2[C@@H]([C@@](N5CCC[C@H]5[C@@](N)=O)=O)[C@](C4=CC=CC=C4Cl)(O)C3=C2C=CC(Cl)=C3)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SR 49059
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 18.61 | 30 |
制备储备液 for SR 49059
以下数据基于产品分子量 620.5。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.3 mM | 5.37 mL | 26.86 mL | 53.72 mL |
| 1.5 mM | 1.07 mL | 5.37 mL | 10.74 mL |
| 3 mM | 0.54 mL | 2.69 mL | 5.37 mL |
| 15 mM | 0.11 mL | 0.54 mL | 1.07 mL |
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产品说明书 for SR 49059
参考文献 for SR 49059
参考文献是支持产品生物活性的出版物。
Serradeil-Le Gal et al (1993) Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors. J.Clin.Invest. 92 224 PMID: 8392086
Tahtaoui et al (2003) Identification of the binding sites of the SR 49059 nonpeptide antagonist into the V1a vasopressin receptor using sulfydryl-reactive ligands and cysteine mutants as chemical sensors. J.Biol.Chem. 278 40010 PMID: 12869559
Serradeil-Le Gal et al (1994) Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes. Biochem.Biophys.Res.Comm. 199 353
If you know of a relevant reference for SR 49059, please let us know.
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关键词: SR 49059, SR 49059 supplier, Selective, orally, active, vasopressin, V1a, receptor, antagonists, V2, Receptors, SR49059, Relcovaptan, Vasopressin, 2310, Tocris Bioscience
6 篇 SR 49059 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SR 49059 的部分引用包括：
Xiao et al (2017) Biased OXTergic Modulation of Midbrain DA Systems. Neuron 95 368 PMID: 28669546
Manaenko et al (2011) Arginine-vasopressin V1a receptor inhibition improves neurologic outcomes following an intracerebral hemorrhagic brain injury. Neurochem Int 58 542 PMID: 21256175
Faraco et al (2014) Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress. Acta Neurochir Suppl 34 852 PMID: 24517977
Zhu et al (2013) Arginine vasopressin enhances cell survival via a G protein-coupled receptor kinase 2/β-arrestin1/extracellular-regulated kinase 1/2-dependent pathway in H9c2 cells. Mol Pharmacol 84 227 PMID: 23690069
Manaenko et al (2011) Post-treatment with SR49059 improves outcomes following an intracerebral hemorrhagic stroke in mice. BMC Neurosci 111 191 PMID: 21725754
Xiao et al (2018) OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons. Elife 7 PMID: 29676731
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.