CD38-IN-8
CD38-IN-8 is a brain-penetrant, orally effective, potent CD38 inhibitor with IC50 values of 2.71 nM and 1.94 nM for mCD38 and hCD38, respectively. CD38-IN-8 achieves non-competitive inhibition by forming a covalent adduct in situ with ADPR in the CD38 active site through its imidazole warhead, thereby blocking NAD+ degradation. CD38-IN-8 can be used for research on central nervous system diseases.
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。
- 分子式: C16H14FN5O3S
- 分子量:375.38
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
mCD38 2.71 nM (IC50) |
hCD38 1.94 nM (IC50) |
体外実験
CD38-IN-8 (compound 16) (1-2 h) inhibits CD38 enzyme activity in a cell-free purified enzyme system (mCD38/hCD38), with IC50 values of 2.71 nM and 1.94 nM, respectively[1].
CD38-IN-8 exhibits minimal or no off-target inhibitory activity in cell-free pure enzyme systems (sirtuins and PARPs)[1].
CD38-IN-8 shows high apparent permeability in hMDR1-transfected MDCK cell monolayers, with an efflux ratio of 0.73[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL |
|---|---|---|---|
| Mice[1] | 0.5 mg/kg | i.v. | 12.9 L/h/kg |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice [1]
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Dosage:3, 10, 30, 100 mg/kg
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Administration:p.o.; once daily for 4 consecutive days; tissues collected 3 h after the last administration
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Result:Dose-dependently increased NAD+ concentrations measured in brain and lung tissue samples.
化学情報
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分子量 375.38
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分子式 C16H14FN5O3S
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SMILES
O=S(N(N=C1)C=C1C2=NC(C3=CN=CN3CCO4)=C4C=C2F)(C5CC5)=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)
CD38-IN-8 関連分類
HY-189708 関連分類
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