GW4869 GW69A, GW554869A
GW4869 (GW69A, GW554869A) 是中性Smase(鞘磷脂酶)的非竞争性抑制剂,IC50为1 μM。它对N-SMase具有选择性,在浓度高达150 μM时对酸性SMase没有抑制作用,它也是一种常见的外泌体抑制剂。
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货号:
TK0459 -
规格:
- 1mg
- 2mg
- 5mg
- 10mg
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价格:
¥0.00
GW4869 (GW69A, GW554869A) 是中性Smase(鞘磷脂酶)的非竞争性抑制剂,IC50为1 μM。它对N-SMase具有选择性,在浓度高达150 μM时对酸性SMase没有抑制作用,它也是一种常见的外泌体抑制剂。
| CAS No. | 6823-69-4 |
| 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. |
| 分子式 | C30H30Cl2N6O2 |
| 分子量 | 577.5 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder, -20°C ,3 years |
| 溶解性数据 | 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) |
| 体内研究 | 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. |
| 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. |
| 纯度及产品资料 | 98% |