| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Velagliflozin specifically targets the sodium-glucose cotransporter 2 (SGLT2), a glucose transporter located primarily in the proximal convoluted tubule of the nephron. By inhibiting SGLT2, velagliflozin reduces renal glucose reabsorption and promotes urinary glucose excretion, thereby lowering blood glucose concentrations. SGLT2 receptors are also present at lower levels in the pancreas, heart, and brain, but the primary antidiabetic mechanism is renal.
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| ln Vitro |
In vitro, velagliflozin proline acts as an orally active SGLT2 inhibitor with antidiabetic activity. It reduces renal glucose reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations. The compound is formed as a co-crystal with L-proline as a monohydrate, with velagliflozin, L-proline, and H2O in 1:1:1 ratios. Specific IC50 values for SGLT2 inhibition are not provided in the search results.
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| ln Vivo |
In cats, velagliflozin (1 mg/kg, oral, single dose) proline lowers respiratory exchange ratio and raises albumin, cholesterol, beta-hydroxybutyrate (BHB), non-esterified fatty acids (NEFA), and urine glucose excretion[1]. By lowering the hyperinsulin response to dietary nonstructural carbohydrates (NSC), velagliflozin (0.3 mg/kg; PO; once daily for 18 days) proline is well tolerated and may regulate insulin dysregulation and prevent diabetes in ponies. inflammation [2].
In vivo, velagliflozin proline (0.3 mg/kg; p.o.; once daily for 18 days) is well tolerated and can improve insulin disorders and prevent laminitis in ponies by reducing the high insulin response to dietary non-structural carbohydrates (NSC). In ZDF rats and Beagle dogs, velagliflozin increases urinary volume and glucose excretion as well as improves blood glucose control. In dogs, the diuretic effect persists for up to approximately 48 hours following a single administration. In cats, once-daily oral administration of velagliflozin (Senvelgo) is indicated for the management of diabetes mellitus. |
| Enzyme Assay |
The specific protocol for assessing SGLT2 binding and inhibition for velagliflozin would use a [14C]-methyl-alpha-D-glucopyranoside (AMG) uptake assay. HEK-293 cells stably expressing human SGLT2 are seeded in 24-well plates. Cells are washed with sodium-free buffer and pre-incubated with assay buffer containing varying concentrations of velagliflozin (0.01-1000 nM) for 15 minutes. [14C]-AMG (100 uM) is added and incubated for 30 minutes at 37degC. Cells are washed with ice-cold PBS, lysed, and the radioactivity is measured. IC50 values are calculated from the concentration-response curve.
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| Cell Assay |
For in vitro cellular assays, primary human renal proximal tubule epithelial cells or MDCK cells expressing SGLT2 are seeded in 24-well plates. Cells are treated with velagliflozin (0.1-1000 nM) in glucose-free medium for 30 minutes, then 2-deoxy-D-glucose (2-DG) uptake is measured using a fluorescent 2-DG analog (2-NBDG). The fluorescence intensity is measured at Ex/Em = 465/540 nm. Inhibition of glucose uptake is calculated relative to untreated control. Cell viability is assessed using the MTT assay to confirm that the observed effects are due to SGLT2 inhibition and not cytotoxicity.
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| Animal Protocol |
An in vivo protocol for velagliflozin uses a Zucker Diabetic Fatty (ZDF) rat model of type 2 diabetes. Male ZDF rats (6-8 weeks old) are administered velagliflozin proline orally by gavage at doses of 0.1-1 mg/kg once daily for 4 weeks. Blood glucose levels are measured weekly using a glucometer, and oral glucose tolerance tests (OGTT) are performed at baseline and at week 4. Twenty-four-hour urinary glucose excretion (UGE) is measured using a metabolic cage. HbA1c levels are measured at the end of the study. For ponies, velagliflozin (0.3 mg/kg, p.o., once daily for 18 days) reduces the high insulin response to dietary non-structural carbohydrates (NSC) and prevents laminitis.
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| ADME/Pharmacokinetics |
Velagliflozin is rapidly absorbed following oral administration. In rats and dogs, velagliflozin was rapidly absorbed following administration via oral gavage of 1 mg/kg. The toxicokinetics of velagliflozin have been evaluated in dogs, with blood samples collected at six timepoints over a 24-hour period on days 1 and 28. Due to the selectivity of velagliflozin for SGLT2, there is no risk of symptomatic hypoglycemia, as glucose reabsorption is balanced by SGLT1. Velagliflozin is not for use in dogs; it is specifically indicated for cats.
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| Toxicity/Toxicokinetics |
Toxicology data for velagliflozin has been evaluated in animal safety studies. There is evidence of a significant increase in urinary volume in rats and dogs following a single administration of velagliflozin. In dogs, this effect persisted for up to approximately 48 hours. Velagliflozin had no adverse effects on cardiovascular function and no relevant effects on CNS function, with only slight effects observed. Euglycemic diabetic ketoacidosis (eDKA) is a notable adverse effect in diabetic cats treated with SGLT2 inhibitors, which may result in death if not treated promptly. Velagliflozin should not be used in cats with insulin-dependent diabetes mellitus or in cats previously treated with insulin.
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| References |
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| Additional Infomation |
Velagliflozin (brand name Senvelgo) is a veterinary drug approved by regulatory authorities for the management of diabetes mellitus in cats. It is not for use in dogs. The approved dosage for cats is 1 mg/kg once daily. Its empirical formula is C28H36N2O8 with a molecular weight of 528.6. Due to its selectivity for SGLT2, there is no risk of symptomatic hypoglycemia in diabetic cats. Velagliflozin proline has also been studied in ponies to improve insulin disorders and prevent laminitis, demonstrating its broader research applications in animal models of metabolic diseases.
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| Molecular Formula |
C28H34N2O7
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|---|---|
| Molecular Weight |
510.578768253326
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| Exact Mass |
510.236
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| CAS # |
1539295-26-5
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| Related CAS # |
Velagliflozin;946525-65-1;Velagliflozin proline hydrate;1661838-94-3
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| PubChem CID |
72736580
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| Appearance |
White to off-white solid-liquid Mixture
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
696
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C1C[C@H](NC1)C(=O)O.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
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| InChi Key |
UWKBFNWQMSGEPG-ZHNCTCHCSA-N
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| InChi Code |
InChI=1S/C23H25NO5.C5H9NO2/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;7-5(8)4-2-1-3-6-4/h1-4,7-8,10,15,19-23,25-28H,5-6,9,12H2;4,6H,1-3H2,(H,7,8)/t19-,20-,21+,22-,23+;4-/m10/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;(2S)-pyrrolidine-2-carboxylic acid
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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: 100 mg/mL (195.86 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 | 1.9586 mL | 9.7928 mL | 19.5856 mL | |
| 5 mM | 0.3917 mL | 1.9586 mL | 3.9171 mL | |
| 10 mM | 0.1959 mL | 0.9793 mL | 1.9586 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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