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Genz-123346 free base 

Cat. No.: HY-12744 Purity: 99.82%
Handling Instructions

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.

For research use only. We do not sell to patients.

Genz-123346 free base Chemical Structure

Genz-123346 free base Chemical Structure

CAS No. : 491833-30-8

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 290 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Genz-123346 free base:

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Description

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.

IC50 & Target

IC50: 14 nM (GM1)[1]

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[2]. Genz-123346(Genz) is an enhancer of autophagy flux[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. 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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

418.57

Formula

C₂₄H₃₈N₂O₄

CAS No.

491833-30-8

SMILES

CCCCCCCCC(N[[email protected]](CN1CCCC1)[[email protected]@H](C2=CC=C(OCCO3)C3=C2)O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (238.91 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3891 mL 11.9454 mL 23.8909 mL
5 mM 0.4778 mL 2.3891 mL 4.7782 mL
10 mM 0.2389 mL 1.1945 mL 2.3891 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (7.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3 mg/mL (7.17 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (7.17 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats: Genz-123346 is dissolved in water. Zucker diabetic fatty rats treated with Genz-123346 (75 mg/kg) for 6 weeks are fasted overnight. The following morning, the fasted rats are anesthetized and injected with 5 units human insulin into the hepatic portal vein. Quadriceps muscle and liver are harvested 2 min after injection and immediately frozen in liquid nitrogen. Insulin receptor is immunoprecipitated. The immunoprecipitates are analyzed by immunoblotting[1].

Mice: C57BL/6 mice are fed on a high-fat (45% of kcal) diet for 8 weeks, obese mice with comparable body weight gain, glucose, and insulin levels are assigned to either the treated or control groups. The mice are then gavaged daily with Genz-123346 or water for 10 weeks[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.82%

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Keywords:

Genz-123346Genz123346Genz 123346OthersInhibitorinhibitorinhibit

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Genz-123346 free base
Cat. No.:
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