2. GPCR/G Protein Immunology/Inflammation
  3. P2Y Receptor NOD-like Receptor (NLR)
  4. P2Y14R antagonist 1

P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis.

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P2Y14R antagonist 1 Chemical Structure

P2Y14R antagonist 1 Chemical Structure

CAS No. : 2728291-29-8

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P2Y14R antagonist 1 Related Antibodies

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Description

P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis[1].
IC50 & Target[1]

P2Y14 Receptor

0.6 nM (IC50)

P2Y2 Receptor

> 100 nM (IC50)

P2Y6 Receptor

89.7 nM (IC50)

P2Y12 Receptor

> 100 nM (IC50)

P2Y1 Receptor

> 100 nM (IC50)

NLRP3

 

In Vitro

P2Y14R antagonist 1 (compound I-17) (2-256 μM, 24 h) shows no significant cytotoxicity in RAW264.7 cells at concentrations below 256 μM[1].
P2Y14R antagonist 1 (10-40 μM, 1 h) can counteract the effects of MSU and LPS, demonstrating anti-gout inflammatory properties[1].
P2Y14R antagonist 1 (10-40 μM, 1 h) acts upstream of the NLRP3 inflammasome assembly, inhibiting subsequent caspase-1 activation and macrophage pyroptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

P2Y14R antagonist 1 Related Antibodies

Cell Viability Assay[1]

Cell Line: RAW264.7 cells
Concentration: 2-256 μM
Incubation Time: 24 h
Result: Only exhibited significant cytotoxicity only at a dose of 256 μM.

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 10-40 μM
Incubation Time: 1 h
Result: Inhibited the expression of NLRP3 and GSDMD in MSU- and LPS-treated RAW264.7 cells.

Immunofluorescence[1]

Cell Line: RAW264.7 cells
Concentration: 10-40 μM
Incubation Time: 1 h
Result: Significantly reduced the formation of ASC specks induced by MSU and LPS.
In Vivo

P2Y14R antagonist 1 (compound I-17) (5-20 mg/mL, i.p., 1 h) can promote the inflammatory response caused by MSU crystal injection-induced acute gouty arthritis in the MSU-induced mouse gout model[1].
1.19
Pharmacokinetic Analysis in MC38 Syngeneic Model[1]

药代动力学分析[1]

P2Y14R antagonist 1 Cmax(g/mL) T1/2 (h) Tmax (h) AUC0-∞ (h⋅ng/mL) CL (L/h/kg) F (%)
i.v. (10 mg/kg) 1533 7.6 18 1765 3.5
p.o. (30 mg/kg) 2895 12.60 32 2845 14.80 75

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Acute gouty arthritis model[1]
Dosage: 5-20 mg/mL
Administration: Intraperitoneal injection (i.p.) , 60 min
Result: Effectively reduced paw swelling in the MSU-induced mouse gout model, significantly decreased the production of pro-inflammatory cytokines IL-1β, IL-6, and IL-18 induced by MSU, markedly inhibited inflammatory cell infiltration in foot tissues induced by MSU, and significantly suppressed the increase of NLRP3 induced by MSU.
Molecular Weight

346.18

Formula

C15H12BrN3O2
CAS No.
SMILES

O=C(NC1=CC2=C(C=C1)N=CN2)COC3=CC=C(C=C3)Br
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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P2Y14R antagonist 1 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:

P2Y14R antagonist 12728291-29-8P2Y ReceptorNOD-like Receptor (NLR)RAW264.7 cellsMouse gout modelGoutInhibitorinhibitorinhibit

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