| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
ZLN024 allosterically promotes the active AMPK heterotrimer and the inactive α1 subunit truncations α1 (1-394) and α1 (1-335), but not α1 (1-312). Activation of AMPK by ZLN024 requires prephosphorylation of Thr-172 by at least one upstream kinase and protects AMPK Thr-172 from dephosphorylation by PP2Cα. ZLN024 activates AMPK in L6 myotubes, promoting glucose uptake and fatty acid oxidation without altering the ADP/ATP ratio. Random screening of AMPK α1β1γ1 heterotrimers utilizing the established scintillation proximity assay (SPA) assay found a novel AMPK activator, ZLN024. ZLN024 directly activates recombinant AMPK α1β1γ1 and its homologue α2β1γ1 in a concentration-dependent manner. ZLN024 raises the activity of α1β1γ1 by 1.5-fold with an EC50 of 0.42 µM and increases the activity of α2β1γ1 by 1.7-fold with an EC50 of 0.95 µM. ZLN024 also directly activates recombinant AMPK α1β2γ1, with an activation effect of 1.7-fold and an EC50 of 1.1 µM; AMPK α2β2γ1 increases by 1.6-fold with an EC50 of 0.13 µM [1].
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|---|---|
| ln Vivo |
For five weeks, C57BKS db/db mice were given ZLN024 at a dose of 15 mg/kg/day by gavage; metformin (Met) at a dose of 250 mg/kg/day served as a positive control. When compared to the vehicle group, food consumption and body weight did not alter significantly during the course of treatment. After four weeks of treatment, ZLN024 enhanced glucose tolerance. ZLN024 15% lowers blood glucose during fasting. Triacylglycerol, total cholesterol, and liver tissue weight are all decreased [1].
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| References |
[1]. Zhang LN, et al. Novel small-molecule AMP-activated protein kinase allosteric activator with beneficial effects in db/db mice. PLoS One. 2013 Aug 20;8(8):e72092
|
| Molecular Formula |
C13H13BRN2OS
|
|---|---|
| Molecular Weight |
325.224120855331
|
| CAS # |
723249-01-2
|
| Related CAS # |
ZLN024 hydrochloride;1883548-91-1
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
CC1=CC=C(OCCSC2=NC=CC=N2)C(Br)=C1
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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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.0748 mL | 15.3742 mL | 30.7484 mL | |
| 5 mM | 0.6150 mL | 3.0748 mL | 6.1497 mL | |
| 10 mM | 0.3075 mL | 1.5374 mL | 3.0748 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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