Physicochemical Properties
| Molecular Formula | C26H29N5O2 |
| Molecular Weight | 443.54 |
| Exact Mass | 443.232 |
| CAS # | 2415643-79-5 |
| PubChem CID | 146673075 |
| Appearance | Typically exists as solid at room temperature |
| LogP | 4.4 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 9 |
| Heavy Atom Count | 33 |
| Complexity | 630 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | HPSVWLBMFVRSNF-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C26H29N5O2/c1-33-18-10-11-23-20(16-18)21(17-32)24(28-23)26-29-22-9-3-2-8-19(22)25(30-26)27-12-4-5-13-31-14-6-7-15-31/h2-3,8-11,16-17,28H,4-7,12-15H2,1H3,(H,27,29,30) |
| Chemical Name | 5-methoxy-2-[4-(4-pyrrolidin-1-ylbutylamino)quinazolin-2-yl]-1H-indole-3-carbaldehyde |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| Targets | AMPK |
| ln Vitro | IQZ23 modifies the activity of ATP synthase, which in turn stimulates the AMPK pathway[1]. After 24 hours of treatment, IQZ23 (0.3 and 1.0 μM) significantly reduces the protein levels of adipogenic factors C/EBPα, PPARγ, and sterol regulatory element-binding protein 1c (SREBP-1c). It also significantly lowers the levels of fatty acid synthesis-related proteins, such as fatty acid synthase (FAS), acetyl CoA carboxylase (ACC), and staroyl-CoA desaturase 1 (SCD1), after 6 days of treatment in 3T3-L1 adipocytes[1]. |
| ln Vivo | Treatment with IQZ23 (20 mg/kg, ip) dramatically reduces body weight increases and associated clinical signs of obesity in mice caused by a high-fat and high-cholesterol diet (HFC) without apparent toxicity[1]. IQZ23, when administered orally (rat 5 mg/kg), shows moderate terminal elimination half-lives (rat 4.2±0.3 h) and Cmax (rat 37.1±7.0 ng/mL)[1]. After being administered intravenously at a dose of 2 mg/kg, IQZ23 shows terminal elimination half-lives (rat 4.4±0.4 h)[1]. |
| Cell Assay |
Western Blot Analysis[1] Cell Types: 3T3-L1 adipocytes Tested Concentrations: 0.3 and 1.0 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished the protein level of adipogenic factors C/EBPα, PPARγ, and SREBP-1c. |
| References |
[1]. Discovery of a Promising Agent IQZ23 for the Treatment of Obesity and Related Metabolic Disorders. Eur J Med Chem. 2020 Apr 15;192:112172. |
Solubility Data
| 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 |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2546 mL | 11.2729 mL | 22.5459 mL | |
| 5 mM | 0.4509 mL | 2.2546 mL | 4.5092 mL | |
| 10 mM | 0.2255 mL | 1.1273 mL | 2.2546 mL |