PD-L1/Nampt-IN-1
PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable KD values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma.
For research use only. We do not sell to patients.
- CAS No.: 3054043-85-2
- Formula: C28H28N4O2
- Molecular Weight:452.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
PD-L1/Nampt-IN-1 (Compound T8) (0.5-5 μM) can enhance the inhibition of the PD-1/PD-L1 interaction in a dose-dependent manner and reachs 76.63% at 5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2 | Tmax | CL | Vz | Cmax | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 3179.2 μg/L·h | 3208.7 μg/L·h | 7.7 h | 8.1 h | 6.4 h | 0.083 h | 1.8 L/h/kg | 17.5 L/kg | 2629.1 μg/L | / |
| Mice[1] | 20 mg/kg | p.o. | 50812.1 μg/L·h | 63324.4 μg/L·h | 3.6 h | 5.4 h | 3.2 h | 0.8 h | 0.6 L/h/kg | 4.3 L/kg | 10822.1 μg/L | 78.8 % |
| Rat[1] | 2 mg/kg | i.v. | 1163.3 μg/L·h | 1629.5 μg/L·h | 3.1 h | 3.6 h | 9.9 h | 0.083 h | 1.2 L/h/kg | 17.4 L/kg | 687.5 μg/L | / |
| Rat[1] | 20 mg/kg | p.o. | 10481.8 μg/L·h | 10491.4 μg/L·h | 7.2 h | 7.2 h | 3.1 h | 3.6 h | 2.4 L/h/kg | 11 L/kg | 951.4 μg/L | 64.4 % |
PD-L1/Nampt-IN-1 is highly concentrated in tumors (1133.6 ng/mL at 8 hours), and penetrates the blood-brain barrier (81.86 ng/mL at 1 hour)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B16-F10 tumor model established in 6–8 weeks old male C57BL/6 mice[1]
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Dosage:50 mg/kg
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Administration:Oral administration (p.o.), for 14 days
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Result:Effectively inhibited melanoma tumor growth with a TGI of 40.1%.
Shows normal fluctuations in mouse body weight during treatment.
Increased the percentage of CD3+, CD3+CD4+, and CD3+CD8+.
No morphological aberration in organ tissues.
Chemical Information
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CAS No. 3054043-85-2
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Molecular Weight 452.55
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Formula C28H28N4O2
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SMILES
COC1=C(C=CC(C2=C(C(C3=CC=CC=C3)=CC=C2)C)=N1)CNCCNC(C4=CN=CC=C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PD-L1/Nampt-IN-1 Related Classifications
HY-175294 Related Classifications
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