CAY10678 - CAS:1268709-57-4

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CAY10678 (Synonyms:mPGES1-IN-7)

目录号 : KCM10888 CAS No. : 1268709-57-4 纯度 : ≥98%

Data Sheet 产品使用指南

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH into the biologically active PGE Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α. CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC = 0.09 and 0.9 µM, respectively). It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration. CAY10678 dose-dependently blocks PGE synthesis in isolated cells and whole blood treated with LPS or IL-1β. It also dose-dependently reduces PGE synthesis and cell recruitment during inflammation in mice.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
1mg		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

CAY10678 is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). CAY10678 reduces PGE2 production and tends to reduce levels of other prostaglandins. CAY10678 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan in mice[1].

IC₅₀&Target

IC50: 0.9 μM (recombinant human mPGES-1), 0.09 μM (recombinant rat mPGES-1)[1]; lipocalin-type PGD synthase (I-PGDS)[1]

体外研究

CAY10678 (0.64-80 μ M; 24 h) can reduce PGE2 production induced by LPS (10 ng/mL) stimulation in A549 cells, mouse macrophages, and blood [1].

CAY10678 inhibits PGE2 synthesis in a concentration dependent manner, leading to the diversion of PGH2 to the prostacyclin pathway [1]

体内研究

CAY10678 (10-100 mg/kg; ip; single dose) effectively inhibits the overall synthesis of prostaglandins and reduces cell migration in a mouse model of balloon inflammation induced by 1% λ - Carrageenan [1].

Animal Model:	1% Carrageenan stimulated mouse air pouch model
Dosage:	10, 50, 100 mg/kg
Administration:	ip; single dose after modeling: use 3 mL of sterile-filtered air was injected sub-cutaneously into the interscapular region of mice; triggered in the pouch 24 h later by the injection of a 1 ml solution of λ-carrageenan (1%) in saline.
Result:	Had no effect on inflammatory exudate volume but dose-dependently reduced cell migration. Resulted in a decrease in PGE2 synthesis, it does not affect changes in other prostaglandin levels, but leads to an overall downregulation of prostaglandin synthesis.

分子式

C₂₃H₃₄N₄O

分子量

382.54

CAS号

1268709-57-4

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

In Vitro:

DMSO : 31.25 mg/mL (81.69 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6141 mL	13.0705 mL	26.1411 mL
5 mM	0.5228 mL	2.6141 mL	5.2282 mL
10 mM	0.2614 mL	1.3071 mL	2.6141 mL

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2 mg/mL (5.23 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (5.23 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

纯度： ≥98%

Data Sheet

产品使用指南

[1]. Leclerc P, et al. Characterization of a human and murine mPGES-1 inhibitor and comparison to mPGES-1 genetic deletion in mouse models of inflammation. Prostaglandins Other Lipid Mediat. 2013 Dec;107:26-34.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器