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Purity: ≥98%
GSK269962 (also known as GSK269962A) is a novel, potent and selective inhibitor of ROCK (Rho-associated protein kinase) with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. GSK269962A induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM), and lowers blood pressure in a rat model of hypertension; GSK269962A represent a novel class of ROCK inhibitors that have profound effects in the vasculature and may enable us to further evaluate the potential beneficial effects of ROCK inhibition in animal models of cardiovascular as well as other chronic diseases.
| ln Vitro |
The half-life of GSK269962A against recombinant human ROCK1 is 1.6 nM. GSK269962A demonstrates selectivity for a panel of serine/threonine kinases that is over 30-fold [1]. With an IC50 of 35 nM, GSK269962A causes vasodilation in the precontracted rat aorta [1].
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| ln Vivo |
GSK269962A is an effective medication for hypertension. In spontaneously hypertensive rats (SHR), GSK269962A (0.3, 1, and 3 mg/kg; oral gavage) causes a dose-dependent drop in blood pressure. Blood pressure is sharply and significantly lowered [1].
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (350-400g)[1]
Doses: 0.3, 1, and 3 mg/kg Route of Administration: po (oral gavage); 12 hrs (hours) Experimental Results: Induced a dose-dependent reduction in blood pressure. |
| References | |
| Additional Infomation |
GSK-269962A is a Rho kinase (ROCK) inhibitor with both ROCK1 and ROCK2 affinity.
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| Molecular Formula |
C29H30N8O5
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| Molecular Weight |
570.60
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| Exact Mass |
570.234
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| CAS # |
850664-21-0
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| Related CAS # |
GSK269962A hydrochloride;2095432-71-4
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| PubChem CID |
16095342
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| Appearance |
White to light yellow solid powder
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| Density |
1.45
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| LogP |
4.431
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
42
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| Complexity |
860
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YOVNFNXUCOWYSG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H30N8O5/c1-2-37-24-17-25(31-18-23(24)33-28(37)26-27(30)35-42-34-26)41-22-5-3-4-20(16-22)32-29(38)19-6-8-21(9-7-19)40-15-12-36-10-13-39-14-11-36/h3-9,16-18H,2,10-15H2,1H3,(H2,30,35)(H,32,38)
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| Chemical Name |
N-[3-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethylimidazo[4,5-c]pyridin-6-yl]oxyphenyl]-4-(2-morpholin-4-ylethoxy)benzamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.65 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7525 mL | 8.7627 mL | 17.5254 mL | |
| 5 mM | 0.3505 mL | 1.7525 mL | 3.5051 mL | |
| 10 mM | 0.1753 mL | 0.8763 mL | 1.7525 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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