Chemical Structure : FR173657
CAS No.:
167838-64-4
FR173657
(FK-3657)
Catalog No.: PC-26638Not For Human Use, Lab Use Only.
FR173657 (FK-3657) is a potent, selective, orally active bradykinin B2 receptor (B2R) antagonist with IC50 of 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
FR173657 (FK-3657) is a potent, selective, orally active bradykinin B2 receptor (B2R) antagonist with IC50 of 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively.
FR173657 displaces[3H]-BK binding to B2 receptors with an IC50 of 2.9 nM and a Ki of 0.36 nM in human lung fibroblast IMR-90 cells.
FR173657 doess not reduce [3H]-des]Arg10-kallidin binding to B1 receptors.
FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg).
FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg).
Physicochemical Properties
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M.Wt
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592.48
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Formula
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C30H27Cl2N5O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(E)-3-(6-Acetamidopyridin-3-yl)-N-(2-((2,4-dichloro-3-(((2-methylquinolin-8-yl)oxy)methyl)phenyl)(methyl)amino)-2-oxoethyl)acrylamide
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References
1. Asano M, et al. Br J Pharmacol. 1997 Feb;120(4):617-24.
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