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LX2761

Cat. No. M9738
LX2761 Structure
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

LX2761 is a locally acting SGLT1 and SGLT2 inhibitor in vitro with IC50 values of 2.2 nM and 2.7 nM for hSGLT1 and hSGLT2, respectively. LX2761 is a very potent, chemically stable, and luminally restricted molecule that achieved proof of concept in OGTT at very low doses. LX2761 was designed to remain in the intestine after oral delivery to inhibit SGLT1 locally without affecting the SGLT1/2 mechanism in the kidney.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 601.8
Formula C32H47N3O6S
CAS Number 1610954-97-6
Purity >98%
Solubility
Storage -20°C, dry, protect from light, sealed
References

Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes
Nicole C Goodwin, et al. J Med Chem. 2017 Jan 26;60(2):710-721. PMID: 28045524.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LX2761 supplier, SGLT, inhibitors

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