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Merck

D1692

Sigma-Aldrich

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′-苯双丙烯酰胺 二盐酸盐

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About This Item

经验公式(希尔记法):
C30H28N6O2 · 2HCl
CAS号:
分子量:
577.50
分類程式碼代碼:
41121800
PubChem物質ID:
NACRES:
NA.77

product name

GW4869, ≥90% (NMR)

品質等級

化驗

≥90% (NMR)

形狀

powder

儲存條件

desiccated
protect from light

顏色

light yellow to yellow

mp

>300 °C

溶解度

DMSO: 0.2 mg/mL

起源

GlaxoSmithKline

儲存溫度

2-8°C

SMILES 字串

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 密鑰

NSFKAZDTKIKLKT-LOLTXFFGSA-N

一般說明

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。

應用

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

特點和優勢

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


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Hasna Ahyayauch et al.
Scientific reports, 8(1), 7456-7456 (2018-05-12)
The mechanisms of Pb(II) toxicity have been studied in human red blood cells using confocal microscopy, immunolabeling, fluorescence-activated cell sorting and atomic force microscopy. The process follows a sequence of events, starting with calcium entry, followed by potassium release, morphological
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)
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
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)
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)

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