(R)-KT109
(R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC50 values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation.
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- CAS 番号: 2055172-60-4
- 分子式: C27H26N4O
- 分子量:422.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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DAGLα 9.1 (pIC50) |
DAGLβ 8.2 (pIC50) |
(R)-KT109 (0.1-1000 nM) selectively inhibits ABHD6 in mouse brain membrane proteome at concentrations ranging from 0.1 to 1000 nM[1].
(R)-KT109 (10 μM; 30 min) inhibits 99% of endogenous DAGLα and 95% of endogenous ABHD6 in mouse brain membrane proteome[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2055172-60-4
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分子量 422.52
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分子式 C27H26N4O
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SMILES
O=C(N1C=C(C2=CC=C(C3=CC=CC=C3)C=C2)N=N1)N4[C@H](CCCC4)CC5=CC=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)