GPR68 antagonist 1
GPR68 antagonist 1 is a GPR68 antagonist with an IC50 of 81 nM. GPR68 antagonist 1 inhibits the mouse GPR68-mediated cAMP signaling pathway with an IC50 of 179 nM. GPR68 antagonist 1 alleviates disease symptoms in a dextran sulfate sodium (DSS) (HY-116282C)-induced mouse model of inflammatory bowel disease. GPR68 antagonist 1 is applicable to research related to inflammatory bowel disease.
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- Fòrmula: C28H24F2O2
- Peso molecular:430.49
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
IL-6 |
IL-1β |
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | CLz/F | Vz/F | AUC0-t | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | 1889.06 ng/mL | 2.00 h | 3.21 h | 2.45 mL/min/kg | 11.40 L/kg | 12243.55 ng·h/mL | / |
| Mice[1] | 30 mg/kg | p.o. | 182.91 ng/mL | 0.50 h | 2.73 h | 51.20 mL/min/kg | 203.18 L/kg | 552.49 ng·h/mL | 2.36 % |
| Mice[1] | 10 mg/kg | i.v. | 1774.50 ng/mL | 0.08 h | 2.51 h | 1.28 mL/min/kg | 4.63 L/kg | 7808.94 ng·h/mL | / |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (6-8 weeks old; DSS-induced IBD model)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.p.; daily; 10 days (day 0 to day 9)
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Result:Delayed weight loss in DSS-exposed mice, with weight recovery observed after switching to normal water.
Reduced colonic shortening.
Prolonged mouse survival.
Mitigated colon tissue damage as shown by H&E staining.
Reduced infiltration of S100A9-positive inflammatory cells in colon tissues.
Significantly decreased serum levels of pro-inflammatory cytokines IL-6, IL-1β, and TNF-α.
Significantly reduced mRNA expression of Il-6, Il-1β, and Tnf-α in colon tissues.
Chemical Information
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Peso molecular 430.49
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Fòrmula C28H24F2O2
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SMILES
FC1=CC=C(CC(C2=CC=C(O)C=C2)C(C3=CC=C(O)C=C3)CC4=CC=C(F)C=C4)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GPR68 antagonist 1 Related Classifications
HY-181485 Related Classifications
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