SQ22536

製品コードS8283 バッチS828301

印刷

化学情報

Chemical Structure 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)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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). This compound 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 in KK/Ta-Akita mice. the amelioration of glomerular histopathological damage is eliminated in KK/Ta-Akita mice treated with this compound. Renal cAMP does not increase after treatment with this chemical. In a word, the beneficial actions 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 this compound 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

  • https://pubmed.ncbi.nlm.nih.gov/11858802/
  • https://pubmed.ncbi.nlm.nih.gov/16332989/
  • https://pubmed.ncbi.nlm.nih.gov/25512345/
  • https://pubmed.ncbi.nlm.nih.gov/25393959/
  • https://pubmed.ncbi.nlm.nih.gov/24152968/

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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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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