2. GPCR/G Protein
  3. P2Y Receptor
  4. 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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MRS4917

MRS4917 Chemical Structure

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MRS4917 Related Antibodies

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Description

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[1].

IC50 & Target[1]

hP2Y14R

2.88 nM (IC50)

P2Y6 Receptor

54 μM (IC50)

In Vitro

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.

MRS4917 Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2 and SH-SY5Y cells
Concentration: 0.1-10 μM
Incubation Time: 72 h
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.
In Vivo

MRS4917 (1.37 and 4.58 mg/kg, p.o and i.p., single dose) reduces mechanoallodynia in CCI mouse model of neuropathic pain[1].
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.

Animal Model: Wild-type C57BL/6J male mice[1]
Dosage: 10 mg/kg
Administration: i.p., single dose
Result: Showed no significant effect on core body temperature.
Induced no significant changes in locomotor activity.
Animal Model: Adult male ICR mice with CCI of the left sciatic nerve (Bennett method)[1]
Dosage: 1.37 mg/kg (p.o.) and 4.58 mg/kg (i.p.)
Administration: p.o. and i.p., single dose
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.
Animal Model: Wild-type C57BL/6J male mice[1]
Dosage: 10 mg/kg
Administration: i.p., 60 min before MRS2905 (5 mg/kg, i.p.)
Result: Blocked the hypothermic effect induced by the P2Y14R agonist MRS2905.
Molecular Weight

458.43

Formula

C27H17F3N2O2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MRS4917 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MRS4917MRS 4917MRS-4917P2Y ReceptorP2Y14RinflammationmechanoallodyniaCCI mouse modelinflammatoryHepG2SH-SY5YInhibitorinhibitorinhibit

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