MRS4917
MRS4917 is an orally active, potent selective P2Y14 receptor (hP2Y14R) antagonist (IC50 = 2.88 nM, Ki = 1.67 nM) that shows >18,000 fold selectivity against P2Y6R (IC50 = 54 μM). MRS4917 demonstrates oral efficacy in reversing established mechanoallodynia in the chronic constriction injury (CCI) mouse model, while having no effect on thermoregulation. MRS4917 can be used for neurological diseases research.
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- Fòrmula: C27H17F3N2O2
- Peso molecular:458.43
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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hP2Y14R 2.88 nM (IC50) |
P2Y6 Receptor 54 μM (IC50) |
MRS4917 (compound 11) (0.1-10 μM, 72 h) demonstrates a favorable in vitro safety profile, showing minimal cytotoxicity, no significant CYP450 inhibition (CYP2D6 or CYP3A4), and high selectivity in a broad off-target panel (only weak activity at α2C receptor)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and SH-SY5Y cells
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Concentration:0.1-10 μM
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Incubation Time:72 h
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Result:Showed low cytotoxicity (18% growth inhibition) in HepG2 cells at 10 μM.
Induced a slight growth-promoting effect (15% increase) in SH-SY5Y cells at 10 μM.
MRS4917 (10 mg/kg, i.p., single dose) shows no effect on body temperature (Tb) or locomotor activity in wild-type C57BL/6J mice[1].
MRS4917 (10 mg/kg, i.p., 60 min before MRS2905) effectively blocks the hypothermic effect induced by the P2Y14R agonist MRS2905 (5 mg/kg, i.p.) in male C57BL/6J mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type C57BL/6J male mice[1]
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Dosage:10 mg/kg
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Administration:i.p., single dose
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Result:Showed no significant effect on core body temperature.
Induced no significant changes in locomotor activity.
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Animal Model:Adult male ICR mice with CCI of the left sciatic nerve (Bennett method)[1]
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Dosage:1.37 mg/kg (p.o.) and 4.58 mg/kg (i.p.)
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Administration:p.o. and i.p., single dose
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Result:Reached full efficacy within 1 hour after both oral and i.p. administration, and maintained this effect over a prolonged period.
The lower oral dose achieved comparable in vivo efficacy to the higher i.p. dose.
Showed no effect on the contralateral (control) paw.
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Animal Model:Wild-type C57BL/6J male mice[1]
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Dosage:10 mg/kg
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Administration:i.p., 60 min before MRS2905 (5 mg/kg, i.p.)
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Result:Blocked the hypothermic effect induced by the P2Y14R agonist MRS2905.
Chemical Information
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Peso molecular 458.43
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Fòrmula C27H17F3N2O2
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SMILES
O=C(O)C1=CC(C2=CC=C(C3=NNC=C3)C=C2)=C4C=CC(C5=CC=C(C(F)(F)F)C=C5)=CC4=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)
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