GW4869 - CAS:6823-69-4 - KKL Med Inc.

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GW4869

目录号 : KM15381 CAS No. : 6823-69-4 纯度 : 95%

Data Sheet SDS 产品使用指南

GW4869 是非竞争性的中性鞘磷脂酶 (N-SMase)抑制剂，IC₅₀值为1 μM。GW4869 是外泌体合成/释放的抑制剂。

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500mg	询价	In-stock

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生物活性

GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC₅₀ of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release.

IC₅₀&Target

IC50: 1 μM (neutral sphingomyelinase)

体外研究

GW4869 (10 μM) partially inhibits TNF-induced sphingomyelin (SM) hydrolysis, and 20 μM of the compound is protected completely from the loss of SM. The addition of 10-20 μM GW4869 completely inhibits the initial accumulation of ceramide, whereas this effect is partially lost at later time points (24 h). The action of GW4869 occurs downstream of the drop in glutathione. GW4869 is able, in a dose-dependent manner, to significantly protect from cell death.
GW4869 (10 or 20 μM) inhibits both exosome release and pro-inflammatory cytokine production in macrophages. GW4869 inhibits the ceramide-mediated inward budding of multivesicular bodies (MVBs) and release of mature exosomes from MVBs.
GW4869 also could reverse the inhibition of CCN2 3’-UTR activity by miR-214-enriched exosomes in hepatic stellate cells.
Solution Attention: GW4869 is routinely stored at −80 °C as a stock suspension in DMSO.

Cell Viability Assay

Cell Line:	MCF7 human breast cancer cells.
Concentration:	10-20 μM.
Incubation Time:	30 min (then treated with TNF (3 nM) followed).
Result:	Significantly inhibited TNF-induced SM hydrolysis, whereas 20 μM of the compound protected completely from the loss of SM.

Cell Viability Assay

Cell Line:	Fresh RAW264.7 macrophages.
Concentration:	10 or 20 μM.
Incubation Time:	2 hours (then treated with 1 μg/mL LPS incubation).
Result:	LPS-triggered exosome generation was remarkably attenuated in macrophages upon pre-treatment of macrophages with 10 μM GW4869, as evidenced by a 22% reduction in the activity of AChE. Such attenuation was further enhanced by treatment with the dose of 20 μM.

体内研究

GW4869 (2.5 μg/g, i.p.) causes inhibition of exosome release blocks LPS-stimulated pro-inflammatory cytokine production and cardiac inflammation in mice. GW4869 mitigates LPS-caused myocardial dysfunction and improves survival in mice.
GW4869 (2.5 μg/g, i.p.) blocks the production of pro-inflammatory cytokines and cardiac inflammation in CLP mice.

Animal Model:	10-12 weeks old Male wild-type C57BL/6 mice (Endotoxin-Challenged Mice).
Dosage:	2.5 μg/g.
Administration:	I.P. once (1 h later, followed by an i.p. injection of LPS (2.5 μg/g, 100 μL)).
Result:	Significantly decreased exosome levels by 37% in sera, compared to levels collected from control mice. At 12 h after LPS injection, the levels of circulating exosomes were increased significantly compared to PBS-controls, as evidenced by a 1.7-fold elevation in the AChE activity.

Animal Model:	10-12 weeks old Male wild-type C57BL/6 mice (CLP Polymicrobial Sepsis Model).
Dosage:	2.5 μg/g.
Administration:	I.P. once (before sham or CLP surgery).
Result:	Decreased exosome concentration by 33% compared to mice injected with PBS in sham-surgery controls. CLP-stimulated exosome release was significantly inhibited by pre-treatment of CLP mice compared to CLP mice pre-treated with PBS.

分子式

C₃₀H₃₀Cl₂N₆O₂

分子量

577.50

CAS号

6823-69-4

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 : 0.1 mg/mL (0.17 mM; Need ultrasonic)

0.1 M HCL : < 1 mg/mL (ultrasonic;adjust pH to 2 with HCl) (insoluble)

H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)

*GW4869 is usually formulated as a suspension.

科研文献

纯度： 95%

Data Sheet

SDS

产品使用指南

暂无相关参考文献

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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KKL 顾客使用本产品发表的 54 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器