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Ertugliflozin L-pyroglutamic acid

Cat. No. M14269
Ertugliflozin L-pyroglutamic acid Structure
Synonym:

PF-04971729 L-pyroglutamic acid

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Biological Activity

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. Has the potential for the treatment of type 2 diabetes mellitus.

Chemical Information
Molecular Weight 566
CAS Number 1210344-83-4
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Vaishali Sahasrabudhe, et al. Relative bioavailability of ertugliflozin tablets containing the amorphous form versus tablets containing the cocrystal form

[2] Andrea Keyter, et al. Can Standardisation of the Public Assessment Report Improve Benefit-Risk Communication?

[3] Beverly Nickerson, et al. Enantioselective analysis for L-pidolic acid in ertugliflozin drug substance and drug product by chiral gas chromatography with derivatization

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Keywords: Ertugliflozin L-pyroglutamic acid, PF-04971729 L-pyroglutamic acid supplier, SGLT, inhibitors, activators


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