| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Velagliflozin targets the sodium-glucose cotransporter 2 (SGLT2), a protein primarily expressed in the proximal tubule of the kidney that is responsible for the majority of glucose reabsorption from the glomerular filtrate. As a SGLT2 inhibitor, it blocks renal glucose reabsorption and promotes glucosuria, thereby lowering blood glucose and insulin concentrations.
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| ln Vitro |
Velagliflozin is an antidiabetic cotransporter of the sodium-glucose cotransporter 2 (SGLT2) family [1].
In vitro, Velagliflozin acts as an SGLT2 inhibitor, blocking glucose transport in cells expressing the transporter. Its activity is assessed using glucose uptake assays in SGLT2-expressing cell lines. The compound's potency is determined by measuring its ability to inhibit sodium-dependent glucose uptake. |
| ln Vivo |
In cats, velagliflozin (1 mg/kg, sidewall, single dose) lowers respiratory exchange and raises albumin, cholesterol, beta-maintaining butyrate (BHB), non-esterified growth (NEFA), and urogenital urgency [1]. By lowering the hyperinsulin response to dietary structural carbohydrates (NSC), velagliflozin (0.3 mg/kg; oral; once daily for 18 days) is well tolerated and can be used to regulate insulin supplementation and avoid laminitis in ponies. [2].
In vivo, Velagliflozin decreases renal glucose reabsorption and promotes glucosuria, thereby lowering blood glucose and insulin concentrations. As an orally available agent, it has been studied in preclinical models of diabetes for its antidiabetic efficacy. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Velagliflozin are performed using membrane preparations expressing human SGLT2. The compound's ability to inhibit sodium-dependent glucose uptake is measured using radiolabeled glucose or fluorescent glucose analogs. The IC50 for inhibition of glucose uptake is calculated from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for Velagliflozin are performed using cells expressing human SGLT2, such as transfected cell lines or renal epithelial cells. Cells are treated with the compound, and glucose uptake is measured using radiolabeled [¹⁴C]-glucose or fluorescent glucose analogs. The inhibition of glucose uptake is quantified, and the IC50 is calculated from concentration-response curves.
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| Animal Protocol |
In vivo animal experiments for Velagliflozin are conducted in rodent models of diabetes, such as db/db mice or streptozotocin-induced diabetic rats. A typical protocol involves oral administration of the compound, followed by measurement of blood glucose levels, urinary glucose excretion, and insulin levels. Efficacy is assessed by comparing glucose-lowering effects between treated and control groups.
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| ADME/Pharmacokinetics |
Velagliflozin has a molecular weight of 395.45 and molecular formula C₂₃H₂₅NO₅. It is an orally available compound. Further PK details, including half-life, bioavailability, and tissue distribution, would be available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Toxicological data for Velagliflozin are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Velagliflozin is an orally available SGLT2 inhibitor with antidiabetic activity. It decreases renal glucose reabsorption and promotes glucosuria, thereby lowering blood glucose and insulin concentrations. This product is for research use only.
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| Molecular Formula |
C23H25NO5
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|---|---|
| Molecular Weight |
395.448306798935
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| Exact Mass |
395.173
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| CAS # |
946525-65-1
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| Related CAS # |
Velagliflozin proline;1539295-26-5;Velagliflozin proline hydrate;1661838-94-3
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| PubChem CID |
24862817
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
648.6±55.0 °C at 760 mmHg
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| Flash Point |
346.1±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.670
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| LogP |
3.87
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
593
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1CC1C2=CC=C(C=C2)CC3=C(C=CC(=C3)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)C#N
|
| InChi Key |
SENUNDCNOYAWGN-ZQGJOIPISA-N
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| InChi Code |
InChI=1S/C23H25NO5/c24-11-17-8-7-16(23-22(28)21(27)20(26)19(12-25)29-23)10-18(17)9-13-1-3-14(4-2-13)15-5-6-15/h1-4,7-8,10,15,19-23,25-28H,5-6,9,12H2/t19-,20-,21+,22-,23+/m1/s1
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| Chemical Name |
2-[(4-cyclopropylphenyl)methyl]-4-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]benzonitrile
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~505.75 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5288 mL | 12.6438 mL | 25.2876 mL | |
| 5 mM | 0.5058 mL | 2.5288 mL | 5.0575 mL | |
| 10 mM | 0.2529 mL | 1.2644 mL | 2.5288 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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