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抑制剂描述:

产品名称:SQ 22536

产品别名:见爱必信官网

英文别名:SQ 22536

靶点:

CAS:17318-31-9

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

SQ 22536 is an A cyclase inhibitor that can permeate the cell. SQ 22536 can block cAMP enhancement mediated by Cordycepin , an inhibitor of human platelet aggregation. In platelet studies SQ 22536 was shown to reverse the antiplatelet effects of Sesamol on p38 MAPK phosphorylation and platelet aggregation, and the stimulatory effects induced by Sesamol on VASP, eNOS phosphorylation, and NO release. SQ 22536 has demonstrated inhibition of the effect of glucagon on rat membrane cyclase activity and has reduced the effect of isoproterenol, epinephrine , norepinephrine, and phenylephrine.

溶解性:DMSO :41 mg/mL (199.79 mM)
Water :41 mg/mL (199.79 mM)
Ethanol :41 mg/mL (199.79 mM)

体外研究:

SQ22536(250 μmol/L) attenuates the inhibitory effect of adenosine against ADP-induced platelet aggregation from 8±5 to 57±5%, respectively (p<0.001). SQ22536 also attenuates an increase of intraplatelet levels of cAMP by adenosine from 29±2 to 9±1 pmol/108 platelets (p<0.05). It has no effect on the platelet antiaggregant activity of inosine (1 to 4 mmol/L) and ADP-induced platelet aggregation.

体内研究:SQ22536 abolishes the renal protective effects of liraglutide in KK/Ta-Akita mice. the amelioration of glomerular histopathological damage by liraglutide is eliminated in KK/Ta-Akita mice treated with liraglutide in combination with SQ22536. Renal cAMP does not increase after treatment with SQ22536. In a word, the beneficial actions of liraglutide for treatment of nephropathy are inhibited by the adenylate cyclase inhibitor SQ22536.

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