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

P2Y14R antagonist 1 Chemical Structure

CAS No. : 2728291-29-8

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  • 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.

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]
1.19
Pharmacokinetic Analysis in MC38 Syngeneic Model[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

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
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (144.43 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8887 mL 14.4434 mL 28.8867 mL
5 mM 0.5777 mL 2.8887 mL 5.7773 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8887 mL 14.4434 mL 28.8867 mL 72.2168 mL
5 mM 0.5777 mL 2.8887 mL 5.7773 mL 14.4434 mL
10 mM 0.2889 mL 1.4443 mL 2.8887 mL 7.2217 mL
15 mM 0.1926 mL 0.9629 mL 1.9258 mL 4.8145 mL
20 mM 0.1444 mL 0.7222 mL 1.4443 mL 3.6108 mL
25 mM 0.1155 mL 0.5777 mL 1.1555 mL 2.8887 mL
30 mM 0.0963 mL 0.4814 mL 0.9629 mL 2.4072 mL
40 mM 0.0722 mL 0.3611 mL 0.7222 mL 1.8054 mL
50 mM 0.0578 mL 0.2889 mL 0.5777 mL 1.4443 mL
60 mM 0.0481 mL 0.2407 mL 0.4814 mL 1.2036 mL
80 mM 0.0361 mL 0.1805 mL 0.3611 mL 0.9027 mL
100 mM 0.0289 mL 0.1444 mL 0.2889 mL 0.7222 mL
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.

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