Physicochemical Properties
| Molecular Formula | C20H21CLN2O3 |
| Molecular Weight | 372.85 |
| CAS # | 3016401-76-3 |
| Appearance | Typically exists as solid at room temperature |
| 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
| ln Vitro | In RAW264, anti-inflammatory agent 64 (2 μM, 4 h) can greatly shield cells and encourage cell growth.H2O2 (0.4 mM) stimulates 7 cells [1]. Nitric oxide (NO) generation in RAW264 can be inhibited by anti-inflammatory drug 64 (2 μM, 24 h) (IC50=0.9 μM).LPS (1 μg/mL) stimulates 7 cells, which has anti-inflammatory properties [1]. When applied to RAW264, anti-inflammatory agent 64 (0.125-2 μM) can drastically decrease ROS protein expression while increasing HO-1.Rot (5 μM) and LPS (1 μM/mL) enhanced 7 cells' protein production, which has antioxidant properties [1]. In a dose-dependent way, anti-inflammatory agent 64 (0.5-2 μM, 24 h) can inhibit TNF-α (IC50=1.52 μM) and IL-6 (IC50=1.73 μM) [1]. The anti-inflammatory drug 64 (0.5-2 μM) has the ability to suppress iNOS protein expression [1]. The NF-κB pathway in RAW264 is inhibited by anti-inflammatory drug 64 (0.5-2 μM).LPS (1 μg/mL) activated 7 cells by preventing IκBα phosphorylation and degradation [1]. |
| ln Vivo | Anti-inflammatory agent 64 (1–30 mg/kg, intraperitoneal injection, gavage, single dose) possesses both antioxidant and anti-inflammatory properties[1]. |
| Cell Assay |
Cell Viability Assay[1] Cell Types: RAW264.7 Tested Concentrations: 2 μM Incubation Duration: 4 h Experimental Results: Could effectively protect the cells treated with LPS, and the cell survival rate is 85%. Could effectively inhibit inflammatory factors ON and had anti -inflammatory properties. |
| Animal Protocol | Animal/Disease Models: Cg-induced mouse paw edema model[1] |
| References |
[1]. Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities. European Journal of Medicinal Chemistry, 2023: 115936. |
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 | 2.6820 mL | 13.4102 mL | 26.8204 mL | |
| 5 mM | 0.5364 mL | 2.6820 mL | 5.3641 mL | |
| 10 mM | 0.2682 mL | 1.3410 mL | 2.6820 mL |