| Size | Price | Stock | Qty |
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| 5mg |
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| ln Vivo |
Remogliflozin etabonate (GSK189075; 10 or 30 mg/kg; oral; twice daily for 6 weeks) significantly reduces FPG and GHb levels in a dose-dependent manner [1]. Remogliflozin etabonate (3, 10, 30 mg/kg; oral) increases urinary glucose excretion in a dose-dependent manner. Remogliflozin etabonate dose-dependently inhibits the increase in plasma glucose and decreases plasma insulin after glucose load in normal rats [1]. Remogliflozin etabonate (1-10 mg/kg; oral) lowers blood glucose and reduces blood glucose AUC for 0-6 hours 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 plasma glucose, plasma insulin and GHb levels in a dose-dependent manner and inhibits the development of hypertriglyceridemia in male GK rats (6 weeks old) [1].
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| Animal Protocol |
Animal/Disease Models: 8weeks old db/db mice[1]
Doses: 10 or 30 mg/kg Route of Administration: Oral; twice (two times) daily for 6 weeks Experimental Results: Dramatically diminished fasting plasma glucose (FPG) in a dose-dependent manner and glycosylated hemoglobin (GHb) levels. Reduce urine output and urinary glucose excretion, and improve hyperglycemia. Urinary Glucose Excretion in Mice and Rats:** Remogliflozin etabonate was suspended in 0.5% sodium carboxymethylcellulose (CMC) and orally administered to female C57BL/6J mice (9 weeks old) and male Sprague-Dawley rats (7 weeks old). After administration, animals were placed in metabolic cages to collect urine for 24 hours. [1] * **Oral Glucose Tolerance Test in Normal and STZ-Induced Diabetic Rats:** Male Sprague-Dawley rats (7 weeks old) or streptozotocin-induced diabetic Wistar rats were fasted for 16 hours. Remogliflozin etabonate (suspended in 0.5% CMC) was administered orally, followed by oral administration of a glucose solution (2 g/kg). Blood samples were collected from the tail vein at specified time points. [1] * **Single Administration in db/db Mice:** Remogliflozin etabonate (suspended in 0.5% CMC) was orally administered to fed male db/db mice (10 weeks old). Blood samples were collected from the tail vein at specified time points. [1] * **Chronic Administration in db/db Mice:** Remogliflozin etabonate (suspended in 0.1% methylcellulose) was orally administered to male db/db mice (8 weeks old) twice a day for 6 weeks. Body weight and food intake were measured every 2 weeks. Fasting blood samples were collected from the tail vein every 2 weeks. At the end of the treatment period, urine was collected over 24 hours using metabolic cages. [1] * **Chronic Administration in High-Fat Diet-Fed GK Rats:** Male GK rats (6 weeks old) were fed a high-fat diet for 4 weeks to induce insulin resistance. They were then fed a high-fat diet containing 0.01%, 0.03%, or 0.1% remogliflozin etabonate for 8 weeks. Blood samples were collected from the tail vein from fed and fasted rats every 4 weeks to monitor parameters. An oral glucose tolerance test (1 g/kg glucose) was performed after 8 weeks of administration. [1] |
| References | |
| Additional Infomation |
Etaponin is a glycoside antibiotic. Etaponin has been used in clinical trials investigating type 2 diabetes and its basic science. Etaponin is an oral prodrug of repaggliflozin, a benzylpyrazole glucoside-based inhibitor of the renal sodium-glucose cotransporter 2 (SGLT2) with hypoglycemic activity. After administration and absorption, the inactive prodrug is converted to the active form repaggliflozin, which selectively acts on sodium-glucose cotransporter 2 (SGLT2).
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| Molecular Formula |
C26H38N2O9
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|---|---|
| Molecular Weight |
522.595
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| Exact Mass |
522.258
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| CAS # |
442201-24-3
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| Related CAS # |
Remogliflozin;329045-45-6
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| PubChem CID |
9871420
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| Appearance |
White to off-white solid powder
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| LogP |
2.509
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
37
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| Complexity |
704
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1[C@H]([C@@H]([C@H]([C@@H]([C@H]1COC(=O)OCC)O)O)O)OC1C(CC2C=CC(=CC=2)OC(C)C)=C(C)N(C(C)C)N=1
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| InChi Key |
UAOCLDQAQNNEAX-ABMICEGHSA-N
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| InChi Code |
InChI=1S/C26H38N2O9/c1-7-33-26(32)34-13-20-21(29)22(30)23(31)25(36-20)37-24-19(16(6)28(27-24)14(2)3)12-17-8-10-18(11-9-17)35-15(4)5/h8-11,14-15,20-23,25,29-31H,7,12-13H2,1-6H3/t20-,21-,22+,23-,25+/m1/s1
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| Chemical Name |
ethyl [(2R,3S,4S,5R,6S)-3,4,5-trihydroxy-6-[5-methyl-1-propan-2-yl-4-[(4-propan-2-yloxyphenyl)methyl]pyrazol-3-yl]oxyoxan-2-yl]methyl carbonate
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| Synonyms |
GSK189075A GSK 189075A GSK-189075A
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~191.35 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.78 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9135 mL | 9.5675 mL | 19.1351 mL | |
| 5 mM | 0.3827 mL | 1.9135 mL | 3.8270 mL | |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9135 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02537470 | COMPLETED | Drug: Biphasic Remogliflozin Etabonate Other: Placebo |
Diabetes Mellitus, Type 2 Type 2 Diabetes Mellitus |
BHV Pharma | 2015-07 | Phase 2 |
| 诊疗号二 | COMPLETED | Drug: Hydrochlorothiazide (HCTZ) Drug: Remogliflozin etabonate (GSK189075) Drug: Furosemide |
Diabetes Mellitus, Type 2 Type 2 Diabetes Mellitus |
GlaxoSmithKline | 2008-03 | Phase 1 |
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