For research use only. Not for therapeutic Use.
Sparsentan（Cat No.:R018917）, also known as RE-021, PS433540 and DARA-a, is a Dual angiotensin II and endothelin A receptor antagonist. Retrophin intends to develop RE-021 for orphan indications of severe kidney diseases including Focal Segmental Glomerulosclerosis (FSGS) as well as conduct proof-of-concept studies in resistant hypertension and diabetic nephropathy. RE-021, with its unique dual blockade of angiotensin and endothelin receptors, is expected to provide meaningful clinical benefits in mitigating proteinuria in indications where there are no approved therapies.
| Catalog Number | R018917 |
| CAS Number | 254740-64-2 |
| Synonyms | 4’-((2-Butyl-4-oxo-1,3-diazaspiro[4.4]non-2-en-1-yl)methyl)-N-(4,5-dimethylisoxazol-3-yl)-2’-(ethoxymethyl)-[1,1’-biphenyl]-2-sulfonamide |
| Molecular Formula | C32H40N4O5S |
| Purity | 98% |
| Target | EDNRA; AGTR2 |
| Target Protein | |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | Ki: 0.8 nM (Human angiotensin II), 9.3 nM (Human endothelin A), 0.4 nM (Rat angiotensin II) |
| IUPAC Name | 2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-(ethoxymethyl)phenyl]-N-(4,5-dimethyl-1,2-oxazol-3-yl)benzenesulfonamide |
| InChI | InChI=1S/C32H40N4O5S/c1-5-7-14-29-33-32(17-10-11-18-32)31(37)36(29)20-24-15-16-26(25(19-24)21-40-6-2)27-12-8-9-13-28(27)42(38,39)35-30-22(3)23(4)41-34-30/h8-9,12-13,15-16,19H,5-7,10-11,14,17-18,20-21H2,1-4H3,(H,34,35) |
| InChIKey | WRFHGDPIDHPWIQ-UHFFFAOYSA-N |
| SMILES | CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC(=C(C=C3)C4=CC=CC=C4S(=O)(=O)NC5=NOC(=C5C)C)COCC |
