| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
NG-497 targets the enzymatically active patatin-like domain of human adipose triglyceride lipase (ATGL, PNPLA2). ATGL is the rate-limiting enzyme for the first step of triglyceride hydrolysis in adipocytes, releasing free fatty acids and glycerol. By selectively inhibiting human and primate ATGL, NG-497 modulates lipolysis and fatty acid metabolism. The compound is inactive against ATGL orthologues from other species, demonstrating species-specific targeting.
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| ln Vitro |
NG-497 removes NG-in human adipocytes in a dose-dependent and reversible way. It does this by selectively inactivating human and non-human primate ATGL while leaving intact structurally and functionally relevant TEG enzymes. In HepG2 cells, 497 (40 μM, 80 min) can decrease lipolysis-dependent respiration without having an off-target effect on mitochondrial function [1].
In vitro, NG-497 dose-dependently inhibits TAG hydrolase activity of human ATGL with an IC50 of 1 μM. In human adipocytes, NG-497 removes triglycerides in a dose-dependent and reversible manner. In HepG2 cells, NG-497 (40 μM, 80 min) decreases lipolysis-dependent respiration without having an off-target effect on mitochondrial function. It selectively inactivates human and non-human primate ATGL while leaving intact structurally and functionally relevant enzymes. |
| ln Vivo |
Specific in vivo data for NG-497 are limited in the available literature. Given its potent and selective ATGL inhibitory activity, the compound has potential for in vivo studies in models of lipid metabolism, obesity, and cancer. Its species specificity (active against human and rhesus monkey, inactive against mouse and rat) limits its use to primate models or humanized systems. The compound is described as a tumor suppressor, suggesting potential for in vivo cancer research.
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| Enzyme Assay |
The ATGL inhibitory activity is assessed using biochemical enzyme assays. Recombinant human ATGL or other species orthologues are incubated with a triglyceride substrate and various concentrations of NG-497. The release of free fatty acids or glycerol is measured, and IC50 values are calculated from dose-response curves. Selectivity is assessed by testing the compound against other lipases and related enzymes.
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| Cell Assay |
For cellular studies, human adipocytes and HepG2 cells are cultured in appropriate media. Cells are treated with NG-497 at various concentrations (e.g., 40 μM for 80 min in HepG2 cells). Triglyceride levels are measured using colorimetric or fluorometric assays. Lipolysis-dependent respiration is assessed by measuring oxygen consumption rates. Mitochondrial function is evaluated using standard assays to confirm lack of off-target effects. Cell viability is assessed using MTT or similar assays.
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| Animal Protocol |
In vivo studies for NG-497 would be conducted in appropriate animal models. However, the compound's species specificity (active against human and rhesus monkey ATGL, inactive against mouse and rat ATGL) presents a challenge for traditional rodent models. Studies would require the use of non-human primates or transgenic mice expressing human ATGL. The compound would be administered via oral gavage or intraperitoneal injection, and endpoints would include triglyceride levels, fatty acid metabolism, and tumor growth.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for NG-497 are not extensively reported. The compound has a molecular weight of 315.36 g/mol, a logP of 3.8, and is soluble in DMSO at ~70 mg/mL (~221.97 mM). It is stored as a powder at -20°C for up to 3 years or in solvent at -80°C for 6 months. Pharmacokinetic studies would be required to determine parameters such as half-life, clearance, and bioavailability in animal models.
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| Toxicity/Toxicokinetics |
NG-497 has been described as non-toxic. In HepG2 cells, it decreases lipolysis-dependent respiration without off-target effects on mitochondrial function. The compound's selectivity for human and primate ATGL over other enzymes suggests a favorable safety profile. However, comprehensive toxicology studies including acute and repeated-dose toxicity assessments have not been reported. The compound should be handled with appropriate safety precautions.
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| References | |
| Additional Infomation |
NG-497 is the first small molecule inhibitor of human and rhesus monkey ATGL (IC50 = 1 μM). It selectively inhibits human and primate ATGL while sparing other species orthologues. The compound has potential value for research on lipid metabolism, obesity, and cancer. No clinical trials or regulatory approvals exist. For research use only.
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| Molecular Formula |
C18H21NO4
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|---|---|
| Molecular Weight |
315.36364531517
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| Exact Mass |
315.147
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| CAS # |
2598242-66-9
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| PubChem CID |
155594277
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
23
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| Complexity |
366
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=CC=C(C=C1)C2=NC(=CC(=C2)OC)C(=O)OC(C)C
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| InChi Key |
VYEIBLWRGBQRPI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21NO4/c1-5-22-14-8-6-13(7-9-14)16-10-15(21-4)11-17(19-16)18(20)23-12(2)3/h6-12H,5H2,1-4H3
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| Chemical Name |
propan-2-yl 6-(4-ethoxyphenyl)-4-methoxypyridine-2-carboxylate
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Solubility (In Vitro) |
DMSO : ~70 mg/mL (~221.97 mM)
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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 | 3.1710 mL | 15.8549 mL | 31.7098 mL | |
| 5 mM | 0.6342 mL | 3.1710 mL | 6.3420 mL | |
| 10 mM | 0.3171 mL | 1.5855 mL | 3.1710 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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