GPR84 antagonist 9
GPR84 antagonist 9 is an orally active GPR84 antagonist with an IC50 value of 12 nM. By antagonizing the GPR84 receptor, GPR84 antagonist 9 blocks immune cell migration, M1 polarization, and the release of inflammatory factors (IL1β/TNFα) induced by medium-chain free fatty acids (MCFFAs) and other substances, thereby comprehensively inhibiting inflammatory and fibrotic responses. GPR84 antagonist 9 can be used in the research of inflammation-driven pain disorders, including neuropathic pain disorders, Fabry disease, gout, and bladder pain syndrome.
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- CAS No.: 2654791-96-3
- Formule: C25H26F3N5O4
- Masse moléculaire:517.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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IL-1β |
TNF-α |
GPR84 antagonist 9 (Compound 320) (0.07 nM-20 μM; 30 min incubation, followed by 30 min agonist stimulation) inhibits Gi-coupled GPR84 receptor activation and restores intracellular cAMP levels in CHO-K1 cells stably expressing the GPR84 receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GPR84 antagonist 9 (10 mg/kg-250 mg/kg; p.o.; once daily; administered from day 10 to day 28) significantly enhances the analgesic effect of increasing mechanical pain threshold in a Streptozotocin (HY-13753)-induced rat model of diabetic neuropathic pain[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley male rats (~9 weeks old) were injected with 2 mg/kg oxaliplatin once daily for 5 days[1]
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Dosage:10 mg/kg, 30 mg/kg, 90 mg/kg
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Administration:p.o.; once daily; starting from day 1 and evaluated up to day 28
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Result:Significantly increased the mechanical paw withdrawal threshold to von Frey filament stimulation, demonstrating analgesic efficacy at doses of 30 mg/kg and 90 mg/kg.
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Animal Model:Sprague Dawley male rats were given 60 mg/kg Streptozotocin (STZ) on day 0[1]
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Dosage:10 mg/kg, 90 mg/kg, 150 mg/kg, 250 mg/kg
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Administration:p.o.; once daily; treated from day 10 up to day 28 post modeling.
Results -
Result:Significantly increased the pain withdrawal threshold to mechanical stimulation in diabetic rats at doses of 90, 150, and 250 mg/kg.
Chemical Information
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CAS No. 2654791-96-3
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Masse moléculaire 517.50
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Formule C25H26F3N5O4
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SMILES
FC(F)(F)C1=C(C(NCC2=NC=C(C3CC3)N=C2)=O)OC4=C1C5=NN(C[C@@H]6OCCOC6)C=C5[C@H](C)C4
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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)
GPR84 antagonist 9 Related Classifications
HY-161682 Related Classifications
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