D1692
GW4869
≥90% (NMR), powder, N-SMase inhibitor
别名:
N,N′-双[4-(4,5-二氢-1H-咪唑-2-基)苯基]-3,3′-对苯双丙烯酰胺 二盐酸盐
产品名称
GW4869, ≥90% (NMR)
质量水平
方案
≥90% (NMR)
表单
powder
储存条件
desiccated
protect from light
颜色
light yellow to yellow
mp
>300 °C
溶解性
DMSO: 0.2 mg/mL
创始人
GlaxoSmithKline
储存温度
2-8°C
SMILES字符串
Cl.Cl.O=C(Nc1ccc(cc1)C2=NCCN2)\C=C/c3ccc(\C=C/C(=O)Nc4ccc(cc4)C5=NCCN5)cc3
InChI
1S/C30H28N6O2.2ClH/c37-27(35-25-11-7-23(8-12-25)29-31-17-18-32-29)15-5-21-1-2-22(4-3-21)6-16-28(38)36-26-13-9-24(10-14-26)30-33-19-20-34-30;;/h1-16H,17-20H2,(H,31,32)(H,33,34)(H,35,37)(H,36,38);2*1H/b15-5-,16-6-;;
InChI key
NSFKAZDTKIKLKT-LOLTXFFGSA-N
一般描述
GW4869是一种常用的抑制外泌体生成的药物。它阻止神经酰胺介导的多泡体(MVBs)向内出芽和成熟外泌体从MVBs释放。GW4869对表达磷脂酰丝氨酸的骨髓瘤细胞具有细胞毒性。它通过浆细胞样树突状细胞(pDCs)而抑制干扰素(干扰素)-α的分泌。
应用
GW4869已可用于：
- 作为中性鞘磷脂酶和外泌体生物发生的抑制剂
- 分析三氧化二砷(ATO)治疗肝癌HCCLM3细胞对神经酰胺生成的影响
- 检测p75神经营养素受体(p75NTR)和原肌球蛋白受体激酶A (TrkA)-偶联通路对神经生长因子(NGF)诱导的大鼠热超敏的影响
生化/生理作用
N-SMase(中性鞘磷脂酶)的一种细胞渗透性、强效、特异性、非竞争性抑制剂
特点和优势
该化合物由 GlaxoSmithKline开发。要浏览其他药物开发的化合物和已批准药物/候选药物的列表，请单击此处。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
Yunlong Huang et al.
Cell discovery, 4, 19-19 (2018-05-01)
Zika virus (ZIKV) is a neurotrophic flavivirus that is capable of infecting humans, leading to brain abnormalities during fetal development. The ZIKV infectivity in neural target cells remains poorly understood. Here, we found that ZIKV specifically infected glial fibrillary acidic
Li Chen et al.
FEBS letters, 590(23), 4263-4274 (2016-10-25)
Exosomes mediate intercellular microRNA delivery between hepatic stellate cells (HSC), the principal fibrosis-producing cells in the liver. The purpose of this study was to identify receptors on HSC for HSC-derived exosomes, which bind to HSC rather than to hepatocytes. Our
Exosomal miR-940 maintains SRC-mediated oncogenic activity in cancer cells: A possible role for exosomal disposal of tumor suppressor miRNAs
Rashed MH, et al.
Oncotarget, 8(12), 20145-20145 (2017)
Laura Hui-Ru Tan et al.
Molecular neurobiology, 55(7), 5741-5756 (2017-10-19)
Sphingomyelinases are a family of enzymes that hydrolyze sphingomyelin to generate phosphocholine and ceramide. The brain distribution and function of neutral sphingomyelinase 2 (nSMase2) were elucidated in this study. nSMase2 mRNA expression was greatest in the striatum, followed by the
Blockade of exosome generation with GW4869 dampens the sepsis-induced inflammation and cardiac dysfunction
Essandoh K, et al.
Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease, 1852(11), 2362-2371 (2015)
商品
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