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Submit ReviewA 127722 is a highly potent and selective ETA endothelin receptor antagonist (IC50 values are 0.11 nM and 98 nM for human ETA and ETB receptors, respectively). Attenuates hypoxia-induced pulmonary hypertension in rats. Orally bioavailable.
A 127722 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 510.62 |
公式 | C29H38N2O6 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 195704-72-4 |
PubChem ID | 159594 |
InChI Key | MOTJMGVDPWRKOC-QPVYNBJUSA-N |
Smiles | O=C(O)[C@@H]1[C@@H](C2=CC=C(OC)C=C2)N(CC(N(CCCC)CCCC)=O)C[C@H]1C3=CC4=C(OCO4)C=C3 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 51.06 | 100 | |
ethanol | 51.06 | 100 |
以下数据基于产品分子量 510.62。 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 |
---|---|---|---|
1 mM | 1.96 mL | 9.79 mL | 19.58 mL |
5 mM | 0.39 mL | 1.96 mL | 3.92 mL |
10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
参考文献是支持产品生物活性的出版物。
Winn et al (1996) 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. J.Med.Chem. 39 1039 PMID: 8676339
Opgenoth et al (1996) Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist. J.Pharmacol.Exp.Ther. 276 473 PMID: 8632312
Chen et al (1997) The orally active nonpeptide endothelin A-receptor antagonist A-127722 prevents and reverses hypoxia-induced pulmonary hypertension and pulmonary vascular remodeling in Sprague-Dawley rats. J.Cardiovasc.Pharmacol 29 713 PMID: 9234651
If you know of a relevant reference for A 127722, please let us know.
关键词: A 127722, A 127722 supplier, A127722, Endothelin, receptor, A, ETA, antagonists, potent, selective, Receptors, 5730, Tocris Bioscience
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