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)
SMILES string
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
assay
≥90% (NMR)
form
powder
storage condition
desiccated
protect from light
color
light yellow to yellow
mp
>300 °C
solubility
DMSO: 0.2 mg/mL
originator
GlaxoSmithKline
storage temp.
2-8°C
Quality Level
Application
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
Biochem/physiol Actions
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
Features and Benefits
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。
General description
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Phillip B Munson et al.
Scientific reports, 9(1), 11688-11688 (2019-08-14)
Malignant mesothelioma (MM) is an asbestos-induced cancer arising on the mesothelial surface of organ cavities. MM is essentially incurable without a means of early diagnosis and no successful standard of care. These facts indicate a deep chasm of knowledge that
The cationic small molecule GW 4869 is cytotoxic to high phosphatidylserine-expressing myeloma cells
Vuckovic S, et al.
British Journal of Haematology, 177(3), 423-440 (2017)
The TrkA receptor mediates experimental thermal hyperalgesia produced by nerve growth factor: modulation by the p75 neurotrophin receptor
Khodorova A, et al.
Neuroscience, 340, 384-397 (2017)
Elevated Wall Tension Leads to Reduced miR-133a in the Thoracic Aorta by Exosome Release
Akerman AW, et al.
Journal of the American Heart Association, 8(1), e010332-e010332 (2019)
Marion Orsini et al.
Cell death and differentiation, 26(9), 1796-1812 (2018-12-14)
Elevated levels of the pro-inflammatory cytokine tumor necrosis factor-α (TNFα) inhibit erythropoiesis and cause anemia in patients with cancer and chronic inflammatory diseases. TNFα is also a potent activator of the sphingomyelinase (SMase)/ceramide pathway leading to ceramide synthesis and regulating
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