货号	规格	价格	上海	北京	珠海	重庆	武汉
S85535-5mg买3赠1	99.30%	￥510.00 S85535-5mg ￥510.00 现货（买3赠1）	7 7	-	-	-	-
S85535-10mg买3赠1	99.30%	￥765.00 S85535-10mg ￥765.00 现货（买3赠1）	6 6	-	-	-	-
S85535-25mg买3赠1	99.30%	￥1530.00 S85535-25mg ￥1530.00 现货（买3赠1）	5 5	-	-	-	-
S85535-100mg	≥98%	￥3600.00 S85535-100mg ￥3600.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

Genz-123346 (free base) is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; inhibits GM1 with IC50 value of 14 nM.

靶点：

IC50: 14 nM (GM1);Glucokinase

体外研究：

Exposure of cells to Genz-123346 and to other GCS inhibitors at nontoxic concentrations can enhance the killing of tumor cells by cytotoxic anti-cancer agents. Genz-123346 and a few other GCS inhibitors are substrates for multi-drug resistance efflux pumps such as P-gp (ABCB1, gP-170). In cell lines selected to over-express P-gp or which endogenously express P-gp, chemosensitization by Genz-123346 is primarily due to the effects on P-gp function. Genz-123346(Genz) is an enhancer of autophagy flux

体内研究：

In the Zucker diabetic fatty rat, Genz-123346 loared glucose and A1C levels and improved glucose tolerance. Drug treatment also prevented the loss of pancreatic beta-cell function and preserved the ability of the animals to secrete insulin. In the diet-induced obese mouse, treatment with Genz-123346 normalized A1C levels and improved glucose tolerance. The oral bioavailability of the drug is shown to be about 10% and 30% in mice and rats, respectively, with a half-life in plasma of 30–60 min. Genz-123346 treatment results in a dose-dependent reduction of renal GlcCer and GM3 levels that translates into effective inhibition of cystic disease. A direct effect of Genz-123346 on the Akt-mTOR signaling pathway is observed, with reduced phosphorylation of Akt and ribosomal protein S6

参考文献：

1. Zhao H, et al. Inhibiting glycosphingolipid synthesis improves glycemic control and insulin sensitivity in animal models of type 2 diabetes. Diabetes. 2007 May;56(5):1210-8. 2. Chai L, et al. The chemosensitizing activity of inhibitors of glucosylceramide synthase is mediated primarily through modulation of P-gp function. Int J Oncol. 2011 Mar;38(3):701-11. 3. Shen W, et al. Inhibition of glucosylceramide synthase stimulates autophagy flux in neurons. J Neurochem. 2014 Jun;129(5):884-94 4. Natoli TA, et al. Inhibition of glucosylceramide accumulation results in effective blockade of polycystic kidney disease in mouse models. Nat Med. 2010 Jul;16(7):788-92.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.389 ml	11.945 ml	23.891 ml
5 mM	0.478 ml	2.389 ml	4.778 ml
10 mM	0.239 ml	1.195 ml	2.389 ml
50 mM	0.048 ml	0.239 ml	0.478 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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Genz-123346 free base