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

P2Y14R antagonist 1 (compound I-17) 是一种强效选择性 P2Y14R 拮抗剂，其 IC50 为 0.6 nM。P2Y14R antagonist 1 表现出强效的 P2Y14R 拮抗活性，以及体内外的有效性和良好的药代动力学特性。P2Y14R antagonist 1 通过NOD样受体家族瘤病毒蛋白 (NLRP3)/ 瘤病毒蛋白D (GSDMD) 信号通路减少炎症因子的释放和细胞焦亡。P2Y14R antagonist 1 有望用于急性痛风性关节炎领域的研究。

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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 相关抗体

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查看 P2Y Receptor 亚型特异性产品:

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P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

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NLRP3 NLRP1 NOD1 NOD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

低于 256 μM 浓度的 P2Y14R antagonist 1 (compound I-17) (2-256 μM, 24小时) 在 RAW264.7 细胞中未显示出显著的细胞毒性[1]。
P2Y14R antagonist 1 (10-40 μM, 1 小时) 可以对抗 Uric acid sodium (HY-B2130A) 和 Lipopolysaccharides (HY-D1056) 的作用，具有抑制痛风性炎症的特性[1]。
P2Y14R antagonist 1 (10-40 μM, 1 小时) 作用于 NLRP3 炎症小体组装的上游，抑制了后续的 caspase-1 激活和巨噬细胞焦亡[1]。

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

P2Y14R antagonist 1 相关抗体:

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.
体内研究
(In Vivo)

P2Y14R antagonist 1 (compound I-17) (5-20 mg/mL，腹腔注射，注射时间1 小时)能够在 Uric acid sodium (HY-B2130A) 诱导的小鼠痛风模型中促进由 Uric acid sodium (HY-B2130A) 晶体注射引起的急性痛风性关节炎的炎症[1]。

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.) , Injection time: 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.
分子量

346.18

Formula

C15H12BrN3O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

P2Y14R antagonist 1 相关分类

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  • 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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