| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
By suppressing the expression of the gluconeogenesis gene, AS1708727 prevents the rise in blood glucose levels [1].
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|---|---|
| ln Vivo |
Oral AS1708727 (30 to 300 mg/kg) lowers triglyceride and blood sugar levels while also having antidiabetic actions [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: Fao cells, derived from H4IIE liver cancer cell line. Tested Concentrations: 0.1-3000μM. Incubation Duration: 18 hrs (hours). Experimental Results: G6Pase and PEPCK mRNA levels diminished in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Sixweeks old db/db mice[1].
Doses: 100-1000 mg/kg (pharmacokinetic/PK/PK analysis). Mode of Route of Administration: Orally. Experimental Results: Cmax) was 26.7 μM and maximum drug concentration time (Tmax) was 0.5 hrs (hrs (hours)) at 300 mg/kg [1]. The liver concentration of AS1708727 is 3.7 to 5.4 times higher than the plasma concentration 0.5-2 hrs (hrs (hours)) after oral administration, indicating good hepatic conversion of AS1708727 [1]. Animal/Disease Models: Diabetic model mouse[1]. Doses: 30 to 300 mg/kg. Route of Administration: Orally, twice (two times) daily for 4 days. Experimental Results: Blood glucose levels were Dramatically diminished at 300 mg/kg [1]. Plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels are Dramatically diminished at 300 mg/kg [1]. G6Pase and PEPCK mRNA levels were Dramatically diminished at doses of 100 and 300 mg/kg [1]. |
| References |
| Molecular Formula |
C24H24CL2N2O2
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|---|---|
| Molecular Weight |
443.3656
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| Exact Mass |
442.121
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| CAS # |
1253226-93-5
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| PubChem CID |
49787159
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| Appearance |
White to off-white solid powder
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| LogP |
6.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
571
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C(C([H])([H])OC2=C([H])C([H])=C([H])C3C([H])=NC([H])=C([H])C2=3)=C(C([H])=C([H])C=1N(C([H])([H])[H])C(C([H])([H])C1([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O)Cl
|
| InChi Key |
OZEZQEPCCWFFJQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H24Cl2N2O2/c1-28(23(29)13-16-5-2-3-6-16)21-10-9-20(25)19(24(21)26)15-30-22-8-4-7-17-14-27-12-11-18(17)22/h4,7-12,14,16H,2-3,5-6,13,15H2,1H3
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| Chemical Name |
2-cyclopentyl-N-[2,4-dichloro-3-(isoquinolin-5-yloxymethyl)phenyl]-N-methylacetamide
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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 : ~41.67 mg/mL (~93.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.69 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 20.8 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: 2.08 mg/mL (4.69 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (4.69 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 | 2.2555 mL | 11.2773 mL | 22.5545 mL | |
| 5 mM | 0.4511 mL | 2.2555 mL | 4.5109 mL | |
| 10 mM | 0.2255 mL | 1.1277 mL | 2.2555 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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