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- MedChemExpress(MCE)
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- HY-12744
- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
491833-30-8
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥792.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥369.0 |
| 规格： | 5 mg | 产品价格： | ￥860.0 |
| 规格： | 10 mg | 产品价格： | ￥1376.0 |
| 规格： | 25 mg | 产品价格： | ￥2475.0 |
| 规格： | 50 mg | 产品价格： | ￥3688.0 |
| 规格： | 100 mg | 产品价格： | ￥4800.0 |
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Genz-123346 free base
CAS No. : 491833-30-8
MCE 国际站：Genz-123346 free base
产品活性：Genz-123346是阻断神经酰胺向GL1转化的GL1合酶的抑制剂；抑制GM1IC50值为14 nM。
研究领域：Others
作用靶点：Others
In Vitro: 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.
In Vivo: 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.
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