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SAR407899

Cat. No. M9678
SAR407899 Structure
Size Price Availability Quantity
5mg USD 59.4  USD66 In stock
10mg USD 90  USD100 In stock
25mg USD 180  USD200 In stock
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Quality Control
Biological Activity

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.

SAR407899 inhibits ROCK-2 better than ROCK-1, with IC50s of 102 ± 19 nM and 276 ± 26 nM, respectively, in the presence of 40 μM ATP. SAR407899 also less potently inhibits PKC-Δ and MSK-1, with IC50s of 5.4 and 3.1 μM, respectively. SAR407899 (0.1, 0.3, 1.0, and 3.0 μM) specifically inhibits the ROCK-mediated phosphorylation of MYPTT696 in HeLa cells stimulated with PHEN, and shows such effects at 1 μM and 10 μM in primary rat aortic smooth muscle cells. SAR407899 (3 μM) completely blocks thrombin-induced shrinkage of human umbilical vein endothelial cells (HUVECs) and stress fiber formation.

SAR407899 (0.01-0.30 mg/kg; i.v.) efficiently reduces pressor responses to vasoconstrictor agents in rats.

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 244.29
Formula C14H16N2O2
CAS Number 923359-38-0
Purity 100.0%
Solubility DMSO ≥ 5 mg/mL
Storage at -20°C
References

Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa
Fabio Guagnini, et al. J Transl Med. 2012 Mar 23;10:59. PMID: 22444253.

Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor
Matthias Lohn, et al. Hypertension. 2009 Sep;54(3):676-83. PMID: 19597037.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SAR407899 supplier, ROCK, inhibitors

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