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KGA-2727 is a potent and selective SGLT1 inhibitor for the treatment of diabete. KGA-2727 inhibited SGLT1 potently and highly selectively in an in vitro assay using cells transiently expressing recombinant SGLTs. KGA-2727 inhibited the absorption of glucose but not that of fructose. It has inhibition constant (Ki) values of 97 and 13,600 nM for human (h) SGLT1 and hSGLT2, respectively.
| ln Vitro |
Good linearity for human SGLT1 and SGLT2 is demonstrated by the Dixon plot study of KGA-2727. Dixon plot results show that KGA-2727 inhibits these SGLTs in a way that is competitive. KGA2727 inhibits SGLT1 and SGLT2's absorption of methyl-D-glucopyranoside (AMG) in a dose-dependent manner [1].
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| ln Vivo |
KGA-2727 decreased the rise in plasma glucose following a glucose load in the oral glucose tolerance test conducted in streptozotocin-induced diabetic rats, suggesting that KGA-2727 ameliorated postprandial hyperglycemia [1]. In Zucker diabetic fat (ZDF) rats, long-term administration of KGA-2727 decreased plasma glucose and glycated hemoglobin levels. KGA-2727 can also improve the morphological alterations of the pancreatic islets and renal distal tubules in ZDF rats, maintaining glucose-stimulated insulin production and lowering urine glucose excretion [1].
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| References |
| Molecular Formula |
C26H40N4O8
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|---|---|
| Molecular Weight |
536.6178
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| Exact Mass |
536.284
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| CAS # |
666842-36-0
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| Related CAS # |
666842-36-0
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| PubChem CID |
10052896
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| Appearance |
White to yellow solid powder
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| LogP |
0.6
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
38
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| Complexity |
719
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1[C@]([H])([C@@]([H])([C@]([H])([C@@]([H])([C@@]1([H])C([H])([H])O[H])O[H])O[H])O[H])OC1C(C([H])([H])C2C([H])=C([H])C(=C([H])C=2C([H])([H])[H])OC([H])([H])C([H])([H])C([H])([H])N([H])C([H])([H])C([H])([H])C(N([H])[H])=O)=C(C([H])(C([H])([H])[H])C([H])([H])[H])N([H])N=1
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| InChi Key |
MDBARDSTXONTFS-MNDUUMEHSA-N
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| InChi Code |
InChI=1S/C26H40N4O8/c1-14(2)21-18(25(30-29-21)38-26-24(35)23(34)22(33)19(13-31)37-26)12-16-5-6-17(11-15(16)3)36-10-4-8-28-9-7-20(27)32/h5-6,11,14,19,22-24,26,28,31,33-35H,4,7-10,12-13H2,1-3H3,(H2,27,32)(H,29,30)/t19-,22-,23+,24-,26+/m1/s1
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| Chemical Name |
3-(3-{4-[3-(beta-D-glucopyranosyloxy)-5-isopropyl-1Hpyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)propionamide
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| Synonyms |
KGA-2727 KGA 2727 KGA2727.
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~372.70 mM)
Ethanol : ~100 mg/mL (~186.35 mM) H2O : ~20 mg/mL (~37.27 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (9.32 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 50.0 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: ≥ 5 mg/mL (9.32 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 50.0 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: ≥ 5 mg/mL (9.32 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 | 1.8635 mL | 9.3176 mL | 18.6352 mL | |
| 5 mM | 0.3727 mL | 1.8635 mL | 3.7270 mL | |
| 10 mM | 0.1864 mL | 0.9318 mL | 1.8635 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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