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| 25mg |
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Purity: ≥98%
ZLN005 is a novel, potent and tissue-specific PGC-1α (peroxisome proliferator-activated receptor-γ coactivator-1α) transcriptional activator. In the PGC-1α promoter reporter assay, ZLN005 potently inhibited luciferases. In L6 myotubes, ZLN005 dose-dependently increased PGC-1α mRNA levels. ZLN005 (10 μM) increased the mRNA levels of cytochrome c oxidase 5b (cox5b), acyl-CoA oxidase, strogen-related receptor α (ERRα), NRF1 and GLUT4. ZLN005 (20 μM) increased glucose uptake and oxidation of palmitic acid by 1.8-fold and 1.28-fold respectively in a dose dependent way.
| ln Vitro |
ZLN005 activates AMPK in a dose-dependent manner during a 24-hour period (2.5 – 20 μM)[1].
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| ln Vivo |
When compared to lean mice, ZLN005 (15 mg/kg; oral; daily; for 4 weeks) decreased fasting and random blood glucose levels. [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: L6 myotubes Tested Concentrations: 2.5, 5, 10, 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependent activation of AMPK. |
| Animal Protocol |
Animal/Disease Models: Eightweeks old db/db mice[1]
Doses: 15 mg/kg Route of Administration: Oral administration; per day for 4 weeks Experimental Results: Random blood glucose and fasting blood glucose levels diminished Dramatically over 4 weeks compared with lean mice . |
| References |
[1]. Zhang LN, et al. Novel small-molecule PGC-1α transcriptional regulator with beneficial effects on diabetic db/db mice. Diabetes. 2013 Apr;62(4):1297-307.
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| Molecular Formula |
C17H18N2
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| Molecular Weight |
250.34
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| CAS # |
49671-76-3
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| Related CAS # |
ZLN005-d4;2410443-42-2;ZLN005-d4 hydrochloride
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| SMILES |
N1([H])C2=C([H])C([H])=C([H])C([H])=C2N=C1C1C([H])=C([H])C(=C([H])C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
LQUNNCQSFFKSSK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18N2/c1-17(2,3)13-10-8-12(9-11-13)16-18-14-6-4-5-7-15(14)19-16/h4-11H,1-3H3,(H,18,19)
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| Chemical Name |
2-(4-(tert-butyl)phenyl)-1H-benzo[d]imidazole
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.2 mg/mL (8.79 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.0 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: ≥ 1.25 mg/mL (4.99 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 12.5 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: ≥ 1.25 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1.67 mg/mL (6.67 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9946 mL | 19.9728 mL | 39.9457 mL | |
| 5 mM | 0.7989 mL | 3.9946 mL | 7.9891 mL | |
| 10 mM | 0.3995 mL | 1.9973 mL | 3.9946 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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