SQ22536

製品コードS8283 バッチS828301

化学情報

	Synonyms	9-(tetrahydrofuran-2-yl)-9h-purin-6-amine	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₉H₁₁N₅O
	分子量	205.22	CAS No.	17318-31-9
Solubility (25°C)*	体外	DMSO	41 mg/mL (199.78 mM)
		Water	41 mg/mL (199.78 mM)
		Ethanol	41 mg/mL (199.78 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine) is an inhibitor of adenylyl cyclase with an IC50 of 1.4 μM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.
in vitro	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^[4].
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^[5].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human leukemic mast cell line(HMC-1) and human umbilical cord blood-derived mast cell(hCBMCs)
	濃度	0.1, 1, 10 mM
	反応時間	30 min
	実験の流れ	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.
動物実験	動物モデル	Male C57BL/6J mice
	投薬量	10 mg/kg
	投与方法	s.c.

参考

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カスタマーフィードバック

: Data from [Data independently produced by , , ONCOLOGY REPORTS, 2017, 37:3572-3580]

: Data from [Data independently produced by , , J Food Sci, 2018, 83(9):2394-2401]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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