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.
| Molecular Weight | 501.65 |
| CAS Number | 247257-48-3 |
| Solubility (25°C) | DMSO ≥ 49 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Akshyaya Pradhan, et al. Fimasartan: A new armament to fight hypertension
[2] Byung-Kwan Lim, et al. Fimasartan for Remodeling after Myocardial Infarction
[4] Hae-Young Lee, et al. Fimasartan: A New Angiotensin Receptor Blocker
| Related Angiotensin Receptor Products |
|---|
| TRV055 hydrochloride
TRV055 hydrochloride, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 hydrochloride is efficacious in stimulating cellular Gq-mediated signaling. |
| (Sar1, Ile4, 8)-Angiotensin II
(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. |
| TRV055
TRV055, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). |
| Alamandine
Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. |
| (Sar1)-Angiotensin II
(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. |
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