Velagliflozin proline hydrate

Cat. No.: HY-109018B: FAQs
Data Sheet Handling Instructions

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Velagliflozin proline hydrate is the clinical form of Velagliflozin (HY-109018). Velagliflozin is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor with antidiabetic activity. Velagliflozin reduces renal glucose reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations.

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

Velagliflozin proline hydrate Chemical Structure

CAS No. : 1661838-94-3

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Other In-stock Forms of Velagliflozin proline hydrate:

Other Forms of Velagliflozin proline hydrate:

Velagliflozin In-stock
Velagliflozin proline In-stock

1 Publications Citing Use of MCE Velagliflozin proline hydrate

•Patent. US20200352968A1.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

SGLT2

In Vitro

Velagliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor, with anti-diabetic activity^[1].

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

In Vivo

Velagliflozin proline hydrate (1 mg/kg; p.o.; single dose) increases cholesterol, albumin, beta-hydroxybutyrate (BHB), nonesterified fatty acids (NEFA), and urinary glucose excretion, and decreases respiratory exchange ratio in cats^[1].
Velagliflozin proline hydrate (0.3 mg/kg; p.o.; once daily for 18 d) is well tolerated and can improve insulin disorders and prevent laminitis in ponies by reducing the high insulin response of dietary non-structural carbohydrates (NSC)^[2].

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

Molecular Weight

528.59

Formula

C₂₈H₃₆N₂O₈

CAS No.

1661838-94-3

SMILES

OC([C@@H]1CCCN1)=O.O[C@H]2[C@H](C3=CC(CC4=CC=C(C5CC5)C=C4)=C(C#N)C=C3)O[C@H](CO)[C@@H](O)[C@@H]2O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (378.37 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	1.8918 mL	9.4591 mL	18.9183 mL
5 mM	0.3784 mL	1.8918 mL	3.7837 mL
10 mM	0.1892 mL	0.9459 mL	1.8918 mL

View the Complete Stock Solution Preparation Table

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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

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: ≥ 5 mg/mL (9.46 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.46 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.46 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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).

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

Handling Instructions (2659 KB)

References

[1]. Hoenig M, et al. Effects of the sodium-glucose cotransporter 2 (SGLT2) inhibitor velagliflozin, a new drug with therapeutic potential to treat diabetes in cats. J Vet Pharmacol Ther. 2018 Apr;41(2):266-273. [Content Brief]

[2]. Meier A, et al. The sodium-glucose co-transporter 2 inhibitor velagliflozin reduces hyperinsulinemia and prevents laminitis in insulin-dysregulated ponies. PLoS One. 2018 Sep 13;13(9):e0203655. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8918 mL	9.4591 mL	18.9183 mL	47.2956 mL
	5 mM	0.3784 mL	1.8918 mL	3.7837 mL	9.4591 mL
	10 mM	0.1892 mL	0.9459 mL	1.8918 mL	4.7296 mL
	15 mM	0.1261 mL	0.6306 mL	1.2612 mL	3.1530 mL
	20 mM	0.0946 mL	0.4730 mL	0.9459 mL	2.3648 mL
	25 mM	0.0757 mL	0.3784 mL	0.7567 mL	1.8918 mL
	30 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5765 mL
	40 mM	0.0473 mL	0.2365 mL	0.4730 mL	1.1824 mL
	50 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.9459 mL
	60 mM	0.0315 mL	0.1577 mL	0.3153 mL	0.7883 mL
	80 mM	0.0236 mL	0.1182 mL	0.2365 mL	0.5912 mL
	100 mM	0.0189 mL	0.0946 mL	0.1892 mL	0.4730 mL