| CAS NO: | 254740-64-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Name: Sparsentan CAS#: 254740-64-2 Chemical Formula: C32H40N4O5S Exact Mass: 592.27194 Molecular Weight: 592.75 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Technical Information | Synonym: RE-021; BMS 346567; RE021; PS-433540; BMS346567; RE 021; PS 433540; DARA-a; BMS-346567 Chemical Name: 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 InChi Key: WRFHGDPIDHPWIQ-UHFFFAOYSA-N InChi Code: 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) SMILES Code: O=S(C1=CC=CC=C1C2=CC=C(CN3C(CCCC)=NC4(CCCC4)C3=O)C=C2COCC)(NC5=NOC(C)=C5C)=O |
| Target | Ki: 0.8 nM (Human angiotensin II), 9.3 nM (Human endothelin A), 0.4 nM (Rat angiotensin II)[1] |
|---|---|
| In Vivo | 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[1]. |
| Animal Admin | Rats: Rats are gavaged with vehicle, and immediately thereafter the first bolus (intravenous) iv injection of angiotensin II served as the control pressor response. Irbesartan (30 μmol/kg) and Sparsentan (30 μmol/kg) are given by oral gavage (po), and the rats are re-challenged with angiotensin II at various intervals up to 240 min. There are 6-8 rats per drug dose. The difference between the maximum blood pressure increase before and after drug is reported as the percent (%) inhibition of the angiotensin II pressor effect[1]. |
| References | [1]. Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9 |
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