| CAS NO: | 17318-31-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| 250mg | 询价 |
| 500mg | 询价 |
| Molecular Weight (MW) | 205.22 |
|---|---|
| Formula | C9H11N5O |
| CAS No. | 17318-31-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 41 mg/mL (199.8 mM) |
| Water: 41 mg/mL (199.8 mM) | |
| Ethanol: 41 mg/mL (199.8 mM) | |
| SMILES | NC1=C2N=CN(C3OCCC3)C2=NC=N1 |
| Synonyms | SQ-22536; SQ22536; SQ 22536; SQ-22,536; SQ22,536; SQ 22,536. NSC 53339; 9-(tetrahydrofuran-2-yl)-9h-purin-6-amine |
| In Vitro | In vitro activity: 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. Kinase Assay: SQ22536 more potently inhibits forskolin-induced Elk activation (IC50=10 μM) than 8-Br-cAMP-induced Elk activation (IC50=170 μM). Cell Assay: HMC-1 cells and hCBMCs are plated in 48-well plates and serum-starved overnight. The next day, cells are preincubated with SQ22536 at the indicated concentrations for 30 min before stimulation with CRH (100 nM for HMC-1 or 1 μM for hCBMC) for 3 min in the presence or absence of SQ22536 in serum-free culture media. Cell lysates are then prepared and assayed for protein kinase A activity using ELISA. |
|---|---|
| In Vivo | 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. |
| Animal model | Male C57BL/6J mice |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; s.c. |
| References | Mol Pharmacol. 2013 Jan;83(1):95-105; Eur J Pharmacol. 2002 Feb 2;436(3):227-33; PLoS One. 2014 Nov 13;9(11):e112741; Kidney Int. 2014 Mar;85(3):579-89. |
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