A 127722

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Description: Highly potent, selective ETA antagonist; orally bioavailable
Chemical Name: rel-(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-3-pyrrolidinecarboxylic acid
Purity: ≥98% (HPLC)

Biological Activity 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.

Compound Libraries for A 127722

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Technical Data for A 127722

M. Wt 510.62
Formula C29H38N2O6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 195704-72-4
PubChem ID 159594
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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for A 127722

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 51.06 100
ethanol 51.06 100

Preparing Stock Solutions for A 127722

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for A 127722

References are publications that support the biological activity of the product.

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

Citations for A 127722

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