PD-L1-IN-6
PD-L1-IN-6 (Compound 16) is an orally active inhibitor for PD-L1 expression in neutrophil by targeting STAT3 with KD of 90.5 nmol/L. PD-L1-IN-6 promotes neutrophil-mediated antifungal immunoresponse.
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- Formule: C21H24Cl2O6S
- Masse moléculaire:475.38
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Stockage:
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
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Activité biologique
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Chemical Information
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Neutrophil | IC50 |
>320 μM
Compound: 16
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Cytotoxicity against mouse neutrophils assessed as reduction in cell viability incubated for 16 hrs by flow cytometry analysis
Cytotoxicity against mouse neutrophils assessed as reduction in cell viability incubated for 16 hrs by flow cytometry analysis
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[PMID: 38526960] |
| Neutrophil | IC50 |
3.76 μM
Compound: 16
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Inhibition of fungal curdlan induced PD-L1 expression in mouse neutrophils assessed as reduction in PD-L1 positive Ly6G positive neutrophils incubated for 16 hrs by flow cytometry analysis
Inhibition of fungal curdlan induced PD-L1 expression in mouse neutrophils assessed as reduction in PD-L1 positive Ly6G positive neutrophils incubated for 16 hrs by flow cytometry analysis
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[PMID: 38526960] |
In Vitro
PD-L1-IN-6 (40 μM) inhibits 80.17% PD-L1 expression at 40 μM without significant cytotoxicity in neutrophil[1].
PD-L1-IN-6 is slight permeable for blood brain barrier, with a pe of 1.22×10-6 cm/s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine neutrophil
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Concentration:40 μM
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Incubation Time:
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Result:Maintained 81.52% cell viability at 40 μM.
In Vivo
Pharmacokinetic Analysis of PD-L1-IN-6 in Sprague-Dawley rats[1]
| route | Dose (mg/kg) | Cmax (ng/mL) | T1/2 (h) | Tmax (h) | AUC0-t (ng·h/mL) | AUC0-inf (ng·h/mL) | CL (mL/min/kg) | MRT0-t (h) | Vss (L/kg) | F (%) |
| po | 10 | 113.52 | 1.46 | 0.33 | 166.57 | 182.25 | - | 1.74 | - | 45.1 |
| iv | 2 | 174.78 | 0.17 | 0.14 | 73.87 | 75.44 | 453.10 | 0.25 | 7.46 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C. albicans infected C57BL/6 mice[1]
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Dosage:50-100 mg/kg
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Administration:p.o. for 3 days
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Result:Inhibited secretion of CXCL1 and CXCL2, and accumulation of neutrophils in bone marrow.
Caused reduced fungal burden and increased infiltrationn rate of neutrophils in kidney.
Chemical Information
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Masse moléculaire 475.38
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Formule C21H24Cl2O6S
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SMILES
O=C1O[C@@H]2[C@@]3([C@@]4([C@](C)(CC[C@H]2[C@@H]1CS(=O)(C5=C(C=CC=C5Cl)Cl)=O)O4)CC[C@]3(O)C)[H]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PD-L1-IN-6 Related Classifications
HY-162399 Related Classifications
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