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。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

P2Y14R antagonist 1 Chemical Structure

P2Y14R antagonist 1 Chemical Structure

CAS No. : 2728291-29-8

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

P2Y14R antagonist 1 相关抗体

Top Publications Citing Use of Products

  • 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 MSU 和 LPS 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，1 小时)能够在 MSU 诱导的小鼠痛风模型中促进由 MSU 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.) , 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

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
P2Y14R antagonist 1
目录号：
HY-161727
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z