| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Targets |
Z16078526 targets two distinct biological pathways. First, it functions as an inhibitor of the vesicular monoamine transporter 2 (VMAT2) with an IC50 of 16 nM against the human transporter expressed in HEK293 cell membranes. Second, it acts as an inducer of mitochondrial uncoupling protein 1 (UCP1), a transmembrane protein located in the inner mitochondrial membrane of brown adipocytes that dissipates the proton gradient to generate heat instead of ATP. UCP1 is the key effector of thermogenesis in brown adipose tissue, and its induction by Z16078526 activates the thermogenic program.
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| ln Vitro |
In vitro, Z16078526 at 10 µM induces endogenous Ucp1 expression in primary mouse brown adipocytes. It promotes p38 MAPK phosphorylation and stimulates lipolysis in these cells. The compound activates thermogenic gene expression and enhances mitochondrial uncoupled respiration in mouse brown adipocytes. As a VMAT2 inhibitor, it demonstrates potent activity with an IC50 of 16 nM. This dual pharmacological profile distinguishes Z16078526 from standard VMAT2 inhibitors like tetrabenazine or lobeline, which do not share its thermogenic properties.
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| ln Vivo |
In vivo, Z16078526 stimulates thermogenesis in mice. When administered at a dose of 1.5 mg/kg, it increases body temperature, confirming its ability to induce whole-body thermogenesis. The compound's in vivo thermogenic effects are reproducible and support its utility as a research tool for studying brown adipose tissue function and metabolic regulation.
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| Enzyme Assay |
The VMAT2 inhibitory activity of Z16078526 is typically assessed using radioligand binding or functional uptake assays with recombinant human VMAT2 expressed in HEK293 cell membranes. The compound is incubated at varying concentrations, and IC50 values are calculated from displacement curves. For UCP1 induction studies, primary mouse brown adipocytes are treated with Z16078526 at 10 µM. Ucp1 mRNA and protein levels are quantified by qRT-PCR and Western blot, respectively. Oxygen consumption rate (OCR) is measured using Seahorse metabolic analyzers to evaluate mitochondrial uncoupled respiration. p38 MAPK phosphorylation is detected by Western blot using phospho-specific antibodies.
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| Cell Assay |
The cellular activity of Z16078526 is evaluated in primary mouse brown adipocytes. Cells are treated with the compound at 10 µM for specified durations, and Ucp1 expression is measured by qRT-PCR and Western blot. Oxygen consumption rate (OCR) is assessed using Seahorse analyzers to measure mitochondrial uncoupled respiration. PKA activity and lipolysis are measured using biochemical assays. These assays collectively characterize the compound's ability to activate the thermogenic program in brown adipocytes.
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| Animal Protocol |
In vivo studies of Z16078526 are conducted in mouse models. Mice are administered the compound at 1.5 mg/kg, and body temperature is monitored as a readout of thermogenesis. Brown adipose tissue is collected for analysis of Ucp1 expression and mitochondrial function. The compound's in vivo thermogenic effects have been validated in multiple studies.
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| ADME/Pharmacokinetics |
Z16078526 has a molecular formula of C18H17N3O4S and a molecular weight of 371.41 g/mol. Its IUPAC name is N-(2,4-dimethoxyphenyl)-2-((4-oxo-1,4-dihydroquinazolin-2-yl)thio)acetamide. The compound is a white to off-white solid powder. It is soluble in DMSO. For storage, the powder can be kept at -20°C for up to 3 years or at 4°C for up to 2 years; in solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Z16078526 are limited, as the compound is intended for research use only and not for human or veterinary use. Standard laboratory safety precautions should be followed when handling this compound. No significant toxicity has been reported in the available literature at the doses used for in vivo studies (1.5 mg/kg).
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| References | |
| Additional Infomation |
Z16078526 was first reported in the Journal of Biological Chemistry (2020) by Vergnes et al., who identified it as a small-molecule inducer of UCP1 and thermogenesis via AKAP1/PKA modulation. The compound uniquely combines potent VMAT2 inhibition (IC50 16 nM) with UCP1-mediated thermogenesis induction. This dual activity positions Z16078526 as a unique tool compound for research programs investigating the intersection of monoamine neurotransmission and thermogenic metabolic regulation. It has been cited in top-tier journals and is available from multiple reputable vendors with certified purity. The compound holds potential for research into obesity, metabolic disorders, and energy homeostasis.
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| Molecular Formula |
C18H17N3O4S
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| Molecular Weight |
371.41
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| Exact Mass |
371.09
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| Elemental Analysis |
C, 58.21; H, 4.61; N, 11.31; O, 17.23; S, 8.63
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| CAS # |
852222-94-7
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| Appearance |
White to off-white solid powder
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| InChi Key |
MHSOAGHWQLCVOI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17N3O4S/c1-24-11-7-8-14(15(9-11)25-2)19-16(22)10-26-18-20-13-6-4-3-5-12(13)17(23)21-18/h3-9H,10H2,1-2H3,(H,19,22)(H,20,21,23)
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| Chemical Name |
N-(2,4-dimethoxyphenyl)-2-((4-oxo-1,4-dihydroquinazolin-2-yl)thio)acetamide
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| Synonyms |
Z16078526; Z-16078526; Z 16078526
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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) |
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 | 2.6924 mL | 13.4622 mL | 26.9244 mL | |
| 5 mM | 0.5385 mL | 2.6924 mL | 5.3849 mL | |
| 10 mM | 0.2692 mL | 1.3462 mL | 2.6924 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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