Remogliflozin etabonate (Synonyms: GSK189075)

Name: Remogliflozin etabonate
Brand: MedChemExpress
SKU: HY-14945
Rating: 4.5 (1 reviews)

Cat. No.: HY-14945 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

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Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with K_i values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.

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

Remogliflozin etabonate Chemical Structure

CAS No. : 442201-24-3

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 115	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 115	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Remogliflozin etabonate:

Remogliflozin Get quote

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Description

IC₅₀ & Target^[1]

hSGLT2

1.95 μM (Ki)

rSGLT2

2.14 μM (Ki)

hSGLT1

43.1 μM (Ki)

rSGLT1

8.57 μM (Ki)

In Vivo

Remogliflozin etabonate (GSK189075; 10 or 30 mg/kg; orally; twice daily for 6 weeks) significantly reduced both the FPG and GHb levels in a dosedependent manner^[1].
Remogliflozin etabonate (3, 10, 30 mg/kg; orally) increases urinary glucose excretion in a dose-dependent manner. Remogliflozin etabonate dose-dependently inhibits the increase in plasma glucose after glucose loading and decreases the plasma insulin in normal rats^[1].
Remogliflozin etabonate (1-10 mg/kg; orally) decreases the blood glucose and reduces the AUC_{0–6 h} for blood glucose in a dose-dependent manner^[1].
Remogliflozin etabonate (high-fat diet containing 0.01, 0.03, or 0.1% remogliflozin etabonate for 8 weeks) reduces the levels of plasma glucose, plasma insulin, and GHb in a dose-dependent manner, and it suppresses the development of hypertriglyceridemia in male GK rats (6 weeks of age)^[1].

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

Animal Model:	db/db mice at the age of 8 weeks^[1]
Dosage:	10 or 30 mg/kg
Administration:	Orally; twice daily for 6 weeks
Result:	Significantly reduced both the fasting plasma glucose (FPG) and glycated hemoglobin (GHb) levels in a dosedependent manner. Reduced both urine volume and urinary glucose excretion with ameliorated the hyperglycemia.

Clinical Trial

Molecular Weight

522.59

Formula

C₂₆H₃₈N₂O₉

CAS No.

442201-24-3

Appearance

Solid

Color

White to off-white

SMILES

CCOC(OC[C@H]1O[C@H]([C@@H]([C@@H](O)[C@@H]1O)O)OC2=NN(C(C)C)C(C)=C2CC3=CC=C(OC(C)C)C=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (191.35 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	1.9135 mL	9.5677 mL	19.1355 mL
5 mM	0.3827 mL	1.9135 mL	3.8271 mL
10 mM	0.1914 mL	0.9568 mL	1.9135 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

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: ≥ 2.5 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.81%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (255 KB) HNMR (288 KB) LCMS (259 KB)

Handling Instructions (2659 KB)

References

[1]. Yoshikazu Fujimori, et al. Remogliflozin Etabonate, in a Novel Category of Selective Low-Affinity Sodium Glucose Cotransporter (SGLT2) Inhibitors, Exhibits Antidiabetic Efficacy in Rodent Models. J Pharmacol Exp Ther. 2008 Oct;327(1):268-76. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9135 mL	9.5677 mL	19.1355 mL	47.8386 mL
	5 mM	0.3827 mL	1.9135 mL	3.8271 mL	9.5677 mL
	10 mM	0.1914 mL	0.9568 mL	1.9135 mL	4.7839 mL
	15 mM	0.1276 mL	0.6378 mL	1.2757 mL	3.1892 mL
	20 mM	0.0957 mL	0.4784 mL	0.9568 mL	2.3919 mL
	25 mM	0.0765 mL	0.3827 mL	0.7654 mL	1.9135 mL
	30 mM	0.0638 mL	0.3189 mL	0.6378 mL	1.5946 mL
	40 mM	0.0478 mL	0.2392 mL	0.4784 mL	1.1960 mL
	50 mM	0.0383 mL	0.1914 mL	0.3827 mL	0.9568 mL
	60 mM	0.0319 mL	0.1595 mL	0.3189 mL	0.7973 mL
	80 mM	0.0239 mL	0.1196 mL	0.2392 mL	0.5980 mL
	100 mM	0.0191 mL	0.0957 mL	0.1914 mL	0.4784 mL

Remogliflozin etabonate Related Classifications

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.

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Remogliflozin etabonate (Synonyms: GSK189075)

Customer Review

Other Forms of Remogliflozin etabonate:

Remogliflozin etabonate Related Antibodies

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Complete Stock Solution Preparation Table

Remogliflozin etabonate Related Classifications

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