DPP9-IN-2
DPP9-IN-2 is a selective, potent and orally active inhibitor of Dipeptidyl Peptidase 9 (DPP9 ) with an IC50 of 12.9 nM. DPP9-IN-2 shows a SI of 59 over DPP8, and shows no significant inhibitory activity against related peptidases including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 can induce cancer cells pyroptosis and has weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitor. DPP9-IN-2 can be used for the researches of cance rand infection.
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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: 3020859-44-0
- 分子式: C33H33F2N3O2
- 分子量:541.63
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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
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DPP-9 12.9 nM (IC50) |
HIV-1 |
DPP9-IN-2 (Compound 6e) (0.05-5 μM; 24-48 h) induces pyroptosis in THP-1 cells, promoting LDH release and SYTOX Green uptake [1].
DPP9-IN-2 (0.5-5 μM; 24 h) induces pyroptosis depending on DPP9, CASP1, and GSDMD, and pyroptosis is significantly inhibited or delayed in DPP9-knockdown, CASP1-KO, or GSDMD-KO THP-1 cells[1].
DPP9-IN-2 (5 μM) shows weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitors (Efavirenz (HY-10572), Rilpivirine (HY-10574)) in MT-4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Note | F | AUC0-last | Cl | Vd | T1/2 |
|---|---|---|---|---|---|---|---|---|
| Rat | 20 mg/kg | p.o. | 文献审核 | 61 % | 8176.1 ng·h/mL | / | / | / |
| Rat | 5 mg/kg | i.v. | 文献审核 | / | 3368.3 ng·h/mL | 1.5 L/h/kg | 23 L/kg | 10.9 h |
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 3020859-44-0
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分子量 541.63
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分子式 C33H33F2N3O2
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SMILES
O=C(C1=CC=C(C2=CC=C(F)C=C2)C=C1)NC34CC5(NCC(N6CC7=C(C=C(F)C=C7)C6)=O)CC(C4)CC(C5)C3
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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)
DPP9-IN-2 関連分類
HY-179348 関連分類
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