GW 4869 (hydrochloride hydrate)|6823-69-4|-陌孚医药/Medlife

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GW 4869 (hydrochloride hydrate)

目录号: PC18138 纯度: ≥98%

CAS No. :6823-69-4

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中文名称	GW 4869 (hydrochloride hydrate)
中文别名	4',4''-双-2-咪唑啉-2-基对苯二丙烯酰苯胺二盐酸盐
英文名称	GW 4869 (hydrochloride hydrate)
英文别名	2-Propenamide,3,3'-(1,4-phenylene)bis[N-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-,dihydrochloride;2-Propenamide,3,3'-(1,4-phenylene)bis[N-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-,dihydrochlor...;GW 4869;GW 4869 (hydrochloride hydrate);GW-4869;Hydrochloride Hydrate;N,N′-Bis[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-3,3′-p-phenylene-bis-acrylamide dihydrochloride;4',4''-Di-2-imidazolin-2-yl-p-benzenediacrylanilide dihydrochloride;GW4869
Cas No.	6823-69-4
分子式	C₃₀H₂₈N₆O₂^.₂[HCl]^.H₂O
分子量	595.52
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

性状

Solid

IC50 & Target[1][2]

IC50: 1 μM (neutral sphingomyelinase)

体外研究(In Vitro)

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.

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

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(In Vivo)

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.

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

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. Luberto C, et al. Inhibition of tumor necrosis factor-induced cell death in MCF7 by a novel inhibitor of neutralsphingomyelinase. J Biol Chem. 2002 Oct 25;277(43):41128-39. [Information]

[2]. Essandoh K, et al. Blockade of exosome generation with GW4869 dampens the sepsis-induced inflammation and cardiac dysfunction. Biochim Biophys Acta. 2015 Nov;1852(11):2362-71. [Information]

[3]. Chen L, et al. Integrins and heparan sulfate proteoglycans on hepatic stellate cells (HSC) are novel receptors for HSC-derived exosomes. FEBS Lett. 2016 Dec;590(23):4263-4274. [Information]

[4]. Nakamura H, et al. Sphingomyelin Regulates the Activity of Secretory Phospholipase A2 in the Plasma Membrane. J Cell Biochem. 2015 Sep;116(9):1898-907. [Information]

溶解度数据	体外研究: 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.

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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