[CAS NO. 1210344-57-2] Ertugliflozin

Name: Ertugliflozin
Brand: Arctom Scientific
SKU: SLK-S5413

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PRODUCTS SPECIFICATIONS [1210344-57-2]

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Catalog

SLK-S5413

Brand

Selleck

CAS

1210344-57-2

DESCRIPTION [1210344-57-2]

Overview

MDL	MFCD21609259
Molecular Weight	436.88
Molecular Formula	C22H25ClO7
SMILES	O[C@H]1[C@@]2(O[C@@](CO)(CO2)[C@@H](O)[C@@H]1O)C3=CC(CC4=CC=C(OCC)C=C4)=C(Cl)C=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2890 mL	11.4448 mL	22.8896 mL
5 mM	0.4578 mL	2.2890 mL	4.5779 mL
10 mM	0.2289 mL	1.1445 mL	2.2890 mL
50 mM	0.0458 mL	0.2289 mL	0.4578 mL

Description

Ertugliflozin (MK-8835, PF-04971729) is a potent and selective inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1.

Targets

hSGLT2 ^[1]
(Cell-free assay)

0.877 nM

In vitro

Ertugliflozin (it is claimed) has a 2000-fold increase in selectivity for human SGLT2 over SGLT1 (IC50: SGLT2 = 0.877 nM vs SGLT1 = 1960 nM) in vitro.

In vivo

Ertugliflozin is rapidly absorbed in preclinical species after oral administration, and it is characterized by low clearance (excreted in the urine in preclinical species) and a moderate steady-state distribution volume. There is low potential for pharmacokinetic interaction of ertugliflozin. Ertugliflozin is well absorbed in humans and eliminated largely via glucuronidation. Ertugliflozin improved glycemic control, body weight and blood pressure in patients with T2DM suboptimally controlled by metformin, and is well-tolerated.

References

[1] Meiyan Jiang, et al. Expert Opin Ther Pat. 2015, 25(11): 1349–1352.

Synonyms

β-L-Idopyranose, 1,6-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-

1,6-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-β-L-idopyranose

Ertugliflozin

PF 04971729-00

PF 04971729

MK 8835