1. GPCR/G Protein Apoptosis
  2. P2Y Receptor Necroptosis
  3. HDL-16

HDL-16 是一种有效的 P2Y14R 拮抗剂,IC50 为 0.3095 nM。HDL-16 通过抑制肠上皮细胞 (IEC) 坏死性凋亡和保护粘膜屏障功能来改善 DSS (HY-116282C) 诱导的结肠炎。

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HDL-16 Chemical Structure

HDL-16 Chemical Structure

CAS No. : 2373280-36-3

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDL-16 is a potent P2Y14R antagonist with an IC50 of 0.3095 nM. HDL-16 ameliorates DSS (HY-116282C)-induced colitis through suppressing necroptosis of intestinal epithelium cells (IECs) and protecting mucosal barrier function[1].

IC50 & Target[1]

P2Y14 Receptor

0.3095 nM (IC50)

体外研究
(In Vitro)

HDL-16 的苯并恶唑环上的 N 原子与 Tyr102 残基形成氢键,胺基也与 P2Y14R 的结合口袋中的 His184 残基形成氢键相互作用[1]
HDL-16 在 10 μM 浓度下对 HT-29 细胞几乎无细胞毒性[1]
HDL-16 可以抑制 HT-29 细胞的坏死性凋亡 (20 ng/mL TNF-α 加 20 μM z-VAD-fmk (HY-16658B) 和 Smac 模拟物 (BV6,2 μM);作用 8 小时)[1]

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

体内研究
(In Vivo)

HDL-16 (10 μM 或 20 μM;100 μL;直肠给药;每天;6 天) 高剂量的可显着抑制小鼠结肠炎症状,并维持小鼠肠道屏障的完整性[1]

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

Animal Model: Male, 7-8-week-old, P2Y14Rfl/fl Vil-cre (P2Y14R∆IEC), P2Y14Rfl/fl Lyz2-cre and WT mice with C57BL/6 J background[1]
Dosage: 10 μM or 20 μM; 100 μL
Administration: Rectally administered; daily; 6 days
Result: With high-dose showed dramatically less body weight loss and lower Disease Activity Index (DAI) than Dextran sodium sulfate (DSS; 36-50 kDa; 3% w/v; drinking water for 7 days)-exposed mice.
With high-dose improved DSS-induced inflammatory infiltration and tissue damage.
With high-dose resulted in a prominently suppression in necroptosis of the IECs in DSS-treated mice.
分子量

303.15

Formula

C14H11BrN2O

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.

溶解性数据
  • 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

In Vivo:

以下溶解方案源自文献,仅供参考,建议您先取少量样品进行尝试。

  • 方案 一

    0.1% DMSO + 99.9% Saline

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
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:
HDL-16
目录号:
HY-161343
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