Genz-123346 free base

SKU: orb1223113

Description

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.

Images & Validation

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Key Properties

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CAS Number	491833-30-8
MW	418.57
Purity	>98% (HPLC)
Formula	C₂₄H₃₈N₂O₄
SMILES	C(=O)(CCCCCCCC)N[C@@H]([C@H](O)c1cc2c(OCCO2)cc1)CN1CCCC1
Target	Gamma-secretase
Solubility	DMSO : ≥ 100 mg/mL; 238.91 mM

Bioactivity

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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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Genz123346 | Genz-123346 | Genz 123346

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Gene Symbol

Gamma-secretase

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