Ertugliflozin (Synonyms: PF-04971729)

Name: Ertugliflozin
Brand: MedChemExpress
SKU: HY-15461
Rating: 5.0 (2 reviews)

Cat. No.: HY-15461 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Ertugliflozin (PF-04971729) 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.

For research use only. We do not sell to patients.

Ertugliflozin Chemical Structure

CAS No. : 1210344-57-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Ertugliflozin:

Ertugliflozin L-pyroglutamic acid In-stock
Ertugliflozin-d₅ Get quote
Ertugliflozin-d₉ Get quote
Ertugliflozin (Standard) Get quote

2 Publications Citing Use of MCE Ertugliflozin

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View All SGLT Isoform Specific Products:

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SGLT1 SGLT2

Biological Activity
Purity & Documentation
References
Customer Review

Description

Ertugliflozin (PF-04971729) 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^[1]. Has the potential for the treatment of type 2 diabetes mellitus^[2].

IC₅₀ & Target

SGLT2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.877 nM Compound: 4, PF-04971729	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr	[PMID: 21449606]
CHO	IC₅₀	1960 nM Compound: 4, PF-04971729	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of methyl alpha-D-glucopyranoside uptake after 1 hr	[PMID: 21449606]

In Vitro

Ertugliflozin (PF-04971729) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

436.88

Formula

C₂₂H₂₅ClO₇

CAS No.

1210344-57-2

Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C([C@]23O[C@@](CO)(CO3)[C@@H](O)[C@H](O)[C@H]2O)C=C1CC4=CC=C(OCC)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (572.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (274 KB) SDS (583 KB)

COA (249 KB) HNMR (268 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54(8):2952-60. [Content Brief]

[2]. Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56. [Content Brief]

[3]. Kalgutkar AS, et al. Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):1609-19. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2890 mL	11.4448 mL	22.8896 mL	57.2240 mL
	5 mM	0.4578 mL	2.2890 mL	4.5779 mL	11.4448 mL
	10 mM	0.2289 mL	1.1445 mL	2.2890 mL	5.7224 mL
	15 mM	0.1526 mL	0.7630 mL	1.5260 mL	3.8149 mL
	20 mM	0.1144 mL	0.5722 mL	1.1445 mL	2.8612 mL
	25 mM	0.0916 mL	0.4578 mL	0.9156 mL	2.2890 mL
	30 mM	0.0763 mL	0.3815 mL	0.7630 mL	1.9075 mL
	40 mM	0.0572 mL	0.2861 mL	0.5722 mL	1.4306 mL
	50 mM	0.0458 mL	0.2289 mL	0.4578 mL	1.1445 mL
	60 mM	0.0381 mL	0.1907 mL	0.3815 mL	0.9537 mL
	80 mM	0.0286 mL	0.1431 mL	0.2861 mL	0.7153 mL
	100 mM	0.0229 mL	0.1144 mL	0.2289 mL	0.5722 mL

Ertugliflozin Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ertugliflozin1210344-57-2PF-04971729PF04971729PF 04971729SGLTSodium-dependent glucose cotransportersInhibitorinhibitorinhibit

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Ertugliflozin (Synonyms: PF-04971729)

Customer Review

Other Forms of Ertugliflozin:

Ertugliflozin Related Antibodies

2 Publications Citing Use of MCE Ertugliflozin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All SGLT Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Ertugliflozin Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Ertugliflozin Related Classifications

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