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Fasudil hydrochloride

Cat. No. M1872
Fasudil hydrochloride Structure
Synonym:

HA-1077; AT877

Size Price Availability Quantity
100mg USD 54  USD60 In stock
200mg USD 74.7  USD83 In stock
500mg USD 121.5  USD135 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 327.83
Formula C14H17N3O2S.HCl
CAS Number 105628-07-7
Purity >99%
Solubility Water ≥60 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Fasudil hydrochloride, HA-1077; AT877 supplier, ROCK, inhibitors

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