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| | Sparsentan (RE-021) Basic information |
| Product Name: | Sparsentan (RE-021) | | Synonyms: | 4'-((2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl)-N-(4,5-dimethylisoxazol-3-yl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide;Sparsentan (RE-021);Sparsentan-d5 (RE-021-d5);RE 201;[1,1'-Biphenyl]-2-sulfonamide, 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-;Sparsentan;4'-[(2-Butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide;BMS-346567 | | CAS: | 254740-64-2 | | MF: | C32H40N4O5S | | MW: | 592.75 | | EINECS: | | | Product Categories: | | | Mol File: | 254740-64-2.mol |  |
| | Sparsentan (RE-021) Chemical Properties |
| Melting point | 148 °C(Solv: isopropanol (67-63-0); water (7732-18-5)) | | Boiling point | 744.4±70.0 °C(Predicted) | | density | 1.28±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: soluble | | form | A crystalline solid | | pka | 7.06±0.50(Predicted) | | 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 | C1(C2=CC=C(CN3C(=O)C4(CCCC4)N=C3CCCC)C=C2COCC)=CC=CC=C1S(NC1C(C)=C(C)ON=1)(=O)=O |
| | Sparsentan (RE-021) Usage And Synthesis |
| Description | Sparsentan (PS-433540, RE-021, DARA) is a dual endothelin type A receptor(ETA) and angiotensin II type 1 receptor antagonist. | | Uses | RE 201 is used an Endothelin A receptor antagonist used in the treatment of hypertension. | | Definition | Sparsentan (RE-021) is a selective dual-acting receptor antagonist with affinity for endothelin (A type) and angiotensin II receptors (Type 1). Sparsentan combines the active moieties of the selective AT1 receptor antagonist irbesartan and a selective ETA receptor antagonist. | | Biological Activity | Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively. | | in vitro | Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED50 value of 0.8 μmol/kg iv and 3.6 μmol/kg po. Sparsentan also shows efficacious and long acting in the big ET-1-induced pressor model. Sparsentan causes a significant lowering of blood pressure at the lowest dose tested (10 μmol/kg/day) in spontaneously hypertensive rats. Sparsentan shows good oral bioavailability in rats, dogs, and monkeys, averaging 40%, 86%, and 21% F, respectively. At 100 μmol/kg/day, Sparsentan reduces the blood pressure from 170 to less than 100 mmHg during the course of the drug’s pharmacokinetic duration. Sparsentan at 100 μmol/kg/day essentially converts the spontaneously hypertensive rats into normotensive rats during the course of its pharmacokinetic duration. |
| | Sparsentan (RE-021) Preparation Products And Raw materials |
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