Genz-123346 is a potent and selective glucosylceramide synthase inhibitor with potential anticancer activity. Exposure of cells to Genz-123346 and to other GCS inhibitors at non-toxic 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 was primarily due to the effects on P-gp function.
CAS Number: 491833-30-8
Molecular Weight: 418.57
Chemical Name: N-[(1R,2R)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl]nonanamide
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Solubility (25°C) DMSO: 84 mg/mL(200.68 mM). Water: Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Zucker diabetic fatty rats, treatment with Genz-123346 significantly lowers blood glucose levels and consequently partially prevents the normal deterioration of pancreatic β-cell function over time and preserves the ability of the islets to secrete insulin. In the high-fat-fed diet-induced obese mice, Genz-123346 essentially normalizes A1C levels to that of the lean animals. The improvement in A1C levels is quite persistent, extending >4 months in the diet-induced obese mice.
- Zhao H, et al. Diabetes. 2007, 56(5):1210-8.
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