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

规格	价格	是否有货
2mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

规格

价格

是否有货

数量

2mg

In-stock

5mg

In-stock

10mg

In-stock

25mg

In-stock

50mg

In-stock

100mg

In-stock

200mg

询价

In-stock

500mg

询价

In-stock

Other Forms of Rapamycin:

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.

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

产品使用指南

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 54 篇科研文献

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