VU6035406
VU6035406 is a functionally selective mAChR inhibitor, with mAChR IC50 values of 21 nM, 51 nM and 47 nM against human, rat and mouse targets, respectively. VU6035406 does not act as a P-glycoprotein substrate. VU6035406 shows extremely low inhibitory activity against cytochrome P450 1A2, 2C9, 2D6 and 3A4. VU6035406 can be used in the research of neurological and psychiatric disorders.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2746405-41-2
- 分子式: C15H16ClN5O3S
- 分子量:381.84
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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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mAChR5 21 |
mAChR5 51 nM (IC50, rat M5 (rM5) |
mAChR5 47 nM (IC50, mouse M5 (mM5)) |
VU6035406 potently inhibits human M5 muscarinic acetylcholine receptor-mediated calcium mobilization in hM5 CHO cells with an IC50 of 21 nM and exhibits >500-fold selectivity over human M1-M4 subtypes[1].
VU6035406 inhibits rat M5 muscarinic acetylcholine receptor-mediated calcium mobilization with an IC50 of 51 nM and exhibits high selectivity over rat M1-M4 subtypes[1].
VU6035406 inhibits mouse M5 muscarinic acetylcholine receptor-mediated calcium mobilization with an IC50 of 47 nM[1].
VU6035406 has a favorable CYP inhibition profile, with no significant inhibition of CYP1A2 or CYP2C9 and weak inhibition of CYP2D6 and CYP3A4[1].
VU6035406 has low to moderate predicted hepatic clearance across multiple species, favorable unbound fractions in plasma and brain, and moderate brain penetration in rats with a Kp,uu of 0.56[1].
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 2746405-41-2
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分子量 381.84
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分子式 C15H16ClN5O3S
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SMILES
O=S(C1=CN=C(C)O1)(N2CCC(CC2)C3=CN4N=CN=C4C=C3Cl)=O
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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)