An AT1 receptor antagonist
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Fimasartan

Item No. 36524

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-butyl-1,6-dihydro-N,N,4-trimethyl-6-oxo-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-5-pyrimidineethanethioamide
CAS Number
247257-48-3
Synonyms
  • BR-A-657
Molecular Formula
C27H31N7OS
Formula Weight
501.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 20 mg/mlEthanol: 0.5 mg/ml
λmax
262 nm
SMILES
O=C1C(CC(N(C)C)=S)=C(C)N=C(CCCC)N1CC2=CC=C(C3=C(C4=NN=NN4)C=CC=C3)C=C2
InChi Code
InChI=1S/C27H31N7OS/c1-5-6-11-24-28-18(2)23(16-25(36)33(3)4)27(35)34(24)17-19-12-14-20(15-13-19)21-9-7-8-10-22(21)26-29-31-32-30-26/h7-10,12-15H,5-6,11,16-17H2,1-4H3,(H,29,30,31,32)
InChi Key
AMEROGPZOLAFBN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Cayman Chemical
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    Product Description

    Fimasartan is an antagonist of the angiotensin II type 1 (AT1) receptor (IC50 = 0.16 nM in HEK293 cells expressing the human receptor).1 It is selective for the AT1- over the AT2 receptor (IC50 = 69 µM). Fimasartan (62.5, 125, and 250 µM) inhibits LPS-induced increases in inducible nitric oxide synthase (iNOS) levels and NO production, as well as NF-κB nuclear translocation in RAW 264.7 macrophages.2 It reduces angiotensin II-induced contractions of isolated rabbit aortic rings in a concentration-dependent manner.1 In vivo, fimasartan decreases mean arterial pressure in rats with hypertension induced by furosemide (Item No. 17273) and renal hypertensive rats when administered at doses of 10 and 0.3 mg/kg, respectively. Formulations containing fimasartan have been used in the treatment of hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chi, Y.H., Lee, J.H., Kim, J.H., et al. Pharmacological characterization of BR-A-657, a highly potent nonpeptide angiotensin II receptor antagonist. Biol. Pharm. Bull. 36(7), 1208-1215 (2013).

    2. Ryu, S., Shin, J.-S., Cho, Y.-W., et al. Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation. Biol. Pharm. Bull. 36(3), 467-474 (2013).