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瀏覽器自帶分享功能也很好用哦~貨號：HY-19363
CAS：6823-69-4
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GW4869
GW4869 是非競爭性的中性鞘磷脂酶 (N-SMase)抑制劑，IC50值為1 μM。GW4869 是外泌體合成/釋放的抑制劑。
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[1][2][3][4].
IC50 & Target
IC50: 1 μM (neutral sphingomyelinase)[1]
體外研究(In Vitro)
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[1].
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[2].
GW4869 also could reverse the inhibition of CCN2 3’-UTR activity by miR-214-enriched exosomes in hepatic stellate cells[3].
Solution Attention: GW4869 is routinely stored at ?80?°C as a stock suspension in DMSO.
Cell Viability Assay[1]
| 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. |
體內(nèi)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[2].
GW4869 (2.5 μg/g, i.p.) blocks the production of pro-inflammatory cytokines and cardiac inflammation in CLP mice[2].
MCE 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)[2]. |
| 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 incr |
分子量：577.50
Formula：C30H30Cl2N6O2
CAS 號：6823-69-4
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式：
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性數(shù)據(jù)
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.
參考文獻
GW4869
GW4869 是非競爭性的中性鞘磷脂酶 (N-SMase)抑制劑，IC50值為1 μM。GW4869 是外泌體合成/釋放的抑制劑。
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[1][2][3][4].
IC50 & Target
IC50: 1 μM (neutral sphingomyelinase)[1]
體外研究(In Vitro)
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[1].
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[2].
GW4869 also could reverse the inhibition of CCN2 3’-UTR activity by miR-214-enriched exosomes in hepatic stellate cells[3].
Solution Attention: GW4869 is routinely stored at ?80?°C as a stock suspension in DMSO.
Cell Viability Assay[1]
| 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. |
體內(nèi)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[2].
GW4869 (2.5 μg/g, i.p.) blocks the production of pro-inflammatory cytokines and cardiac inflammation in CLP mice[2].
MCE 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)[2]. |
| 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 incr |
分子量：577.50
Formula：C30H30Cl2N6O2
CAS 號：6823-69-4
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式：
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性數(shù)據(jù)
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.
參考文獻
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