Bioactivity | CaMKP inhibitor sodium is a selective inhibitor of ROCK1 with an IC50 value of 14 nM. |
Target | IC50: 14 nM (ROCK1). |
Invitro | CaMKP inhibitor sodium at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. CaMKP inhibitor sodium is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). CaMKP inhibitor sodium slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. CaMKP inhibitor sodium significantly inhibits rat aortic ring dilation with IC50 of 190 nM[2]. 0 --> CaMKP inhibitor sodium 相关抗体: |
In Vivo | CaMKP inhibitor sodium has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of CaMKP inhibitor sodium at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg[1]. |
Name | CaMKP inhibitor sodium |
CAS | 52789-62-5 |
Formula | C10H8NNaO7S2 |
Molar Mass | 341.29 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9. [2]. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J. 2009 Oct 23;424(1):47-60. |