A 127722

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Cat.No. 5730 - A 127722 | C29H38N2O6 | CAS No. 195704-72-4
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

M. Wt 510.62
Formula C29H38N2O6
Storage Store at -20°C
Purity ≥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

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

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 510.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, A127722, Endothelin, receptor, A, ETA, antagonists, potent, selective, Endothelin, ETA, Receptors, Endothelin, ETA, Receptors, Tocris Bioscience

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