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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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Enavogliflozin (DPW-16001), an antidiabetic compound, is a first class selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor with oral activity.

Remogliflozin etabonate (GSK189075)

Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.

Bexagliflozin (EGT1442)

Bexagliflozin (EGT1442, EGT-0001442, THR-1442) is a potent and selective SGLT2 inhibitor with an IC50 of 2 nM.

KGA-2727

KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.

Tofogliflozin (hydrate)

Tofogliflozin (CSG-452) hydrate is a potent and highly specific sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 value of 2.9 nM.

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

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