Fimasartan
Cat. No: CDIA-0826
CAS. No.: 247257-48-3
Synonyms: BR-A-657
Size: 5 mg
Product Details |
Formula |
C27H31N7OS |
Molecular Weight |
501.65 |
Appearance |
Solid |
Purity |
98.04% |
Smiles String |
O=C1N(C(CCCC)=NC(C)=C1CC(N(C)C)=S)CC2=CC=C(C3=C(C4=NN=NN4)C=CC=C3)C=C2 |
Storage & Handling |
Shipping |
Room temperature. |
Storage Powder |
-20 °C/3 years, 4 °C/2 years |
Description
Fimasartan(BR-A-657) is a non-peptide angiotensin II receptor antagonist used for the treatment of hypertension and heart failure.
IC50 value:
Target: AT1 receptor antagonist
in vitro: Fimasartan suppressed the expressions of inducible nitric oxide synthase (iNOS) by down-regulating its transcription, and subsequently inhibited the productions of nitric oxide (NO). In addition, fimasartan attenuated LPS-induced transcriptional and DNA-binding activities of nuclear factor-kappa B (NF-κB) and activator protein-1 (AP-1) . BR-A-657 displaced [125I][Sar1
-Ile8]angiotensin II (Ang II) from its specific binding sites to AT1 subtype receptors in membrane fractions of HEK-293 cells with an IC50 of 0.16 nM .
in vivo: After oral administration of 240 mg fimasartan, the mean area under the plasma concentration-time curve from time zero to infinity was 2899.0 ng/ml/h in the older, which was significantly greater than in young subjects (1767.4 ng/ml/h; p = 0.03) . Compared with atorvastatin alone, coadministration of fimasartan and atorvastatin increased the atorvastatin acid mean (95% confidence interval) maximum concentration (Cmax,ss) by 1.89-fold (1.49-2.39) and the area under the concentration curve (AUCτ,ss) by 1.19-fold (0.96-1.48). Fimasartan also increased the mean 2-hydroxy atorvastatin acid Cmax,ss and AUCτ,ss by 2.45-fold (1.80-3.35) and 1.42-fold (1.09-1.85), respectively .
! For research use only. Not intended for any clinical use.
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