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.
For research use only. We do not sell to patients.
- Formula: C27H17F3N2O2
- Molecular Weight:458.43
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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
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Biological Activity
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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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Molecular Weight 458.43
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Formula 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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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)
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