SQ 22536CAS号： 17318-31-9分子式：
C9H11N5O
分子量： 205.22描述纯度储存/保存方法形态别名外观密度熔点沸点折射率IC50PK值Ki 数据可溶性/溶解性MDLPubChem CID靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 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. |
| 纯度 |
≥98%
|
| 储存/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.
|
| 形态 |
Solid
|
| 基本信息 | |
| 别名 |
9-THF-Ade； 9-(tetrahydrofuran-2-yl)-9h-purin-6-amine
|
| 外观 |
white to off-white solid
|
| 密度 |
~1.7 g/cm3 (Predicted)
|
| 熔点 |
171.94° C (Predicted)
|
| 沸点 |
~474.8° C at 760 mmHg (Predicted)
|
| 折射率 |
n20D 1.83
|
| IC50 |
PTH-stimulation of adenylate cyclase: IC50 = 200 µM; cAMP production induced by prostaglandin E1: IC50 = 82 µM (platelet lysates); cAMP production induced by prostaglandin E1: IC50 = 1 µM (intact platelets); Adenylyl cyclase: IC50 = 1.4 µM; PI4-kinase alpha subunit: IC50 = 28.2 µM (human)
|
| PK值 |
pKb: 3.82
|
| Ki 数据 |
Adenosine A2b receptor: Ki= 2400 nM (Rattus norvegicus); PI4-kinase type II beta: Ki= 21.2 µM (human); PI4-kinase alpha subunit: Ki= 21.2 µM (human); Adenosine A1 receptor: Ki= 28 µM (Rattus norvegicus); Adenosine A2b receptor: Ki= 23 (Rattus norvegicus)
|
| 可溶性/溶解性 |
DMSO ：41 mg/mL (199.79 mM)
Water ：41 mg/mL (199.79 mM) Ethanol ：41 mg/mL (199.79 mM) |
| MDL |
MFCD00210216
|
| PubChem CID |
5270
|
| 生物活性 | |
| 靶点 |
adenylate cyclase
|
| In vitro(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.
|
| In vivo(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.
|
分子结构图
