SAR-407899
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $745 | Check With Us |
| 500mg | $1150 | Check With Us |
| 1g | $1725 | Check With Us |
: Cat #: V3093 CAS #: 923359-38-0 Purity ≥ 98%
Description: SAR407899 is a novel, potent, selective, and ATP-competitive ROCK inhibitor with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
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| Molecular Weight (MW) | 244.29 |
|---|---|
| Molecular Formula | C14H16N2O2 |
| CAS No. | 923359-38-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent |
| Protocol | In Vitro | SAR407899 is a potent and ATP-competitive ROCK inhibitor, with 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 concentration-dependently inhibits 5-bromodeoxyuridine incorporation into the cells with an IC50 of 5.0 ± 1.3 μM. SAR407899 also effectively inhibits THP-1 migration with an IC50 of 2.5 ± 1.0 μM. SAR407899 shows a potent vasorelaxant activity in a broad variety of isolated arteries taken from different vascular beds and species, with a range of IC50 values between 122 and 280 nM |
|---|---|---|
| In Vivo | SAR407899 (3 mg/kg, i.v.) inhibits ROCK-mediated phosphorylation of MYPTT696 in thoracic aorta of spontaneously hypertensive rats (SHRs). SAR407899 (0.01-0.30 mg/kg, i.v.) efficiently reduces pressor responses to vasoconstrictor agents in rats. SAR407899 (1, 3, 10, and 30 mg/kg, p.o.) dose dependently lowers blood pressure in hypertensive SHRs |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 4.0935 mL | 20.4675 mL | 40.9350 mL | 81.8699 mL |
| 5mM | 0.8187 mL | 4.0935 mL | 8.1870 mL | 16.3740 mL |
| 10mM | 0.4093 mL | 2.0467 mL | 4.0935 mL | 8.1870 mL |
| 20mM | 0.2047 mL | 1.0234 mL | 2.0467 mL | 4.0935 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
+
%ddH2O
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.