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| 25mg |
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Purity: ≥98%
AM-2394 is a novel, potent and selective Glucokinase activator/agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate. AM-2394 activates GK with an EC50 of 60 nM, increases the affinity of GK for glucose by approximately 10-fold, exhibits moderate clearance and good orally bioavailable bioavailability in multiple animal models, and lowers glucose excursion following an orally bioavailable glucose tolerance test in an ob/ob mouse model of diabetes.
| ln Vivo |
AM-2394 is a physically unique glucokinase activator that dramatically decreases plasma glucose at a dose of 3 mg/kg in the oral glucose tolerance test (OGTT) in ob/ob mice. AM-2394 improves the affinity of glucokinase (GK) for glucose by about 10-fold, demonstrates moderate clearance and acceptable oral bioavailability in numerous animal models, and is fed orally in a diabetic ob/ob mice model Reduce glucose excursions during glucose tolerance tests. AM-2394 displays good to moderate plasma clearance, volume of distribution and oral bioavailability across species and can be further studied in animal models [1].
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| References |
| Molecular Formula |
C22H25N5O4
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|---|---|
| Molecular Weight |
423.4650
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| Exact Mass |
423.19
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| CAS # |
1442684-77-6
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| Related CAS # |
1442684-77-6
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| PubChem CID |
71603585
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| Appearance |
White to off-white solid powder
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| LogP |
1.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
578
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1C([H])=C([H])C(=C([H])N=1)C1=C([H])N=C(C([H])=C1OC1=C([H])N=C([H])C(C([H])([H])[H])=C1[H])N([H])C(N([H])C([H])([H])[H])=O)C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])O[H]
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| InChi Key |
QUISANLDBDCMPD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25N5O4/c1-14-7-16(11-24-9-14)31-18-8-19(27-21(28)23-4)25-12-17(18)15-5-6-20(26-10-15)30-13-22(2,3)29/h5-12,29H,13H2,1-4H3,(H2,23,25,27,28) SMILES
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| Chemical Name |
1-(6'-(2-hydroxy-2-methylpropoxy)-4-((5-methylpyridin-3-yl)oxy)-[3,3'-bipyridin]-6-yl)-3-methylurea
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| Synonyms |
AM-2394 AM 2394 AM2394.
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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 : ≥ 30 mg/mL (~70.84 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.90 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 (5.90 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 (5.90 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 | 2.3614 mL | 11.8072 mL | 23.6144 mL | |
| 5 mM | 0.4723 mL | 2.3614 mL | 4.7229 mL | |
| 10 mM | 0.2361 mL | 1.1807 mL | 2.3614 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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