Fasudil is cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor with an IC50 of 10.7 μM. It is also a Ca2+ antagonist and vasodilator. It also inhibits proliferation of vascular smooth muscle cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 5 mg/mL|
|Related ROCK Products|
SAR407899 is a potent and selective, ATP-competitive ROCK inhibitor with IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
Belumosudil mesylate (SLx-2119 mesylate) is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively).
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
SLx-2119, also known as KD-025, is an orally bioavailable inhibitor of ROCK-II with IC50 of 105 nM.
ZINC00881524 is a potent and selective ROCK inhibitor.
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