Fasudil hydrochloride is a cyclic nucleotide-dependent Rho-associated kinase inhibitor with IC50 of 10.7 μM. The Rho-kinase (ROCK) plays an important role in mediating vasoconstriction and vascular remodeling in the pathogenesis of PH. ROCK increases ACE expression and activity in PH. By inhibiting ROCK with fasudil, circulating ACE and Ang-II are reduced, leading to a decrease in pulmonary vascular pressure, thus decreasing MLC phosphatase activity and enhancing vascular smooth muscle contraction. Fasudil effectively inhibited ISO-induced heart failure, as evaluated by biometric, hemodynamic, and histological examinations. More over, fasudil significantly decreased ISO-induced JNK activation, ERK translocation to the nucleus and subsequent c-fos, c-jun expression and upregulated c-FLIP(L) expression.
|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||Water ≥60 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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