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Genz-123346

Chemical Structure : Genz-123346

CAS No.: 943344-58-9

Genz-123346 (Genz123346)

Catalog No.: PC-43171Not For Human Use, Lab Use Only.

Genz-123346 is a potent, specific glucosylceramide synthase inhibitor with IC50 of 14 nM (GM1 inhibition), does not inhibit α-glucosidase or glucocerebrosidase and little effect on 1-O-acylceramide synthase activity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Genz-123346 is a potent, specific glucosylceramide synthase inhibitor with IC50 of 14 nM (GM1 inhibition), does not inhibit α-glucosidase or glucocerebrosidase and little effect on 1-O-acylceramide synthase activity; effectively inhibits GL1 synthase activity and does not significantly elevate cell ceramide levels in vitro, lowers glucose and A1C levels , and improves glucose tolerance in the Zucker diabetic fatty rats; effectively inhibits cystogenesis in mouse models of polycystic kidney disease (PKD).

Physicochemical Properties

M.Wt 987.2259
Formula C52H82N4O14
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Nonanamide, N-[(1R,2R)-2-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]-, (2R,3R)-2,3-dihydroxybutanedioate (2:1)

References

1. Zhao H, et al. Diabetes. 2007 May;56(5):1210-8.

2. Zhao H, et al. Hepatology. 2009 Jul;50(1):85-93.

3. Natoli TA, et al. Nat Med. 2010 Jul;16(7):788-92.

4. Chai L, et al. Int J Oncol. 2011 Mar;38(3):701-11.

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