A 127722

Pricing Availability   Qty
说明: Highly potent, selective ETA antagonist; orally bioavailable
化学名: rel-(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-3-pyrrolidinecarboxylic acid
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 for A 127722

A 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.

化合物库 for A 127722

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。

技术数据 for A 127722

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.

溶解性数据 for A 127722

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 51.06 100
ethanol 51.06 100

制备储备液 for A 127722

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for A 127722

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


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关键词: A 127722, A 127722 supplier, A127722, Endothelin, receptor, A, ETA, antagonists, potent, selective, Receptors, 5730, Tocris Bioscience

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