Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewA 127722
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
A 127722 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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 |
| 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.
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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets for A 127722
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
If you know of a relevant reference for A 127722, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: A 127722, A 127722 supplier, A127722, Endothelin, receptor, A, ETA, antagonists, potent, selective, Receptors, 5730, Tocris Bioscience
Citations for A 127722
Citations are publications that use Tocris products.
Currently there are no citations for A 127722. Do you know of a great paper that uses A 127722 from Tocris? Please let us know.
Reviews for A 127722
There are currently no reviews for this product. Be the first to review A 127722 and earn rewards!
Have you used A 127722?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image