GW4869|cas:6823-69-4|西域试剂

GW4869,98.86%

产品编号：Bellancom-19363| CAS NO：6823-69-4| 分子式：C₃₀H₃₀Cl₂N₆O₂| 分子量：577.50

GW4869是非竞争性的中性鞘磷脂酶抑制剂，IC50值为1 μM。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-19363	￥900.00	杭州北京（现货）
Bellancom-19363	￥1300.00	杭州北京（现货）
Bellancom-19363	￥2200.00	杭州北京（现货）
Bellancom-19363	￥4600.00	杭州北京（现货）
Bellancom-19363	￥7900.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

GW4869

产品介绍

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。

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^[4].

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.

西域 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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

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.

运输条件

Room temperature in continental US; may vary elsewhere.

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

. 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. [Content Brief]

. 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. [Content Brief]

. 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. [Content Brief]

[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. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

个人防护装备	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
危险品运输编码	NONH for all modes of transport

1. 物质的识别

产品名：	GW4869 2HCl
CAS号：	6823-69-4
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	GW4869 2HCl
别名：	GW69A; GW554869A
分子式：	C30H30Cl2N6O2
分子量：	577.50

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[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.

[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.

[3]. 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.

GW4869,98.86%

GW4869

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

在线咨询