| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CIAC101 inhibited the excessive production of NO in Lipopolysaccharides (LPS)-induced microglia BV-2 with an IC50 value of 17 nM[1]. CIAC101 (0.1 nM-10 μM; 24 h) dose-dependently inhibited LPS-induced NF-κB activation (IC50 of 65.5 nM) and reduced the expression of pro-inflammatory mediators in HEK-BluehTLR4 cells. CIAC101 did not show significant cytotoxicity[1]. In the BV-2 NF-κB luciferase reporter cell line, CIAC101 (0.1 nM-10 μM; 24 h) dose-dependently inhibited LPS-induced NF-κB activation without significant cytotoxicity, with an IC50 of 90.2 nM[1]. In the LPS-stimulated BV-2 microglia model, CIAC101 (0.01-1 μM; 24 h) reduced LPS-induced mRNA expression of iNOS, IL-1β, TNF-α and IL-6 in a concentration-dependent manner [1].
|
|---|---|
| ln Vivo |
CIAC101 (0.005-0.2 mg/kg, intraperitoneal injection, day 4 to day 10) effectively counteracts methamphetamine (METH)-induced neurobehavioral and cognitive changes and neurotrophic factors in mice (Balb/c) [1]. CIAC101 (20 mg/kg; intraperitoneal injection; once daily; for 14 days) was well tolerated in the Balb/c model, with no acute systemic or organ toxicity observed.
|
| Cell Assay |
RT-PCR[1]
Cell Types: BV-2 microglial were treated with 200 ng/mL LPS Tested Concentrations: 0.01 μM, 0.1 μM, 1 μM Incubation Duration: 24 h Experimental Results: Reduced LPS-evoked mRNA expression of iNOS, IL-1β, TNF-α, and IL-6. |
| Animal Protocol |
Animal/Disease Models: Male Balb/c mice (6-8 weeks; 22-25 g) (METH-induced neuroinflammation and addiction-like behaviors)[1]
Doses: 0.005 mg/kg, 0.02 mg/kg, 0.2 mg/kg Route of Administration: Intraperitoneal (i.p.) Experimental Results: Significantly reduced METH-induced behavioral sensitization and conditioned place preference (CPP). Also attenuated microglial activation and proinflammatory gene expression (IL-1β, TNF-α, and IL-6) in the medial prefrontal cortex (mPFC) and ventral tegmental area (VTA). |
| References |
| Molecular Formula |
C24H29NO4
|
|---|---|
| Molecular Weight |
395.49
|
| Appearance |
Typically exists as solids 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)
|
| 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
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 | 2.5285 mL | 12.6425 mL | 25.2851 mL | |
| 5 mM | 0.5057 mL | 2.5285 mL | 5.0570 mL | |
| 10 mM | 0.2529 mL | 1.2643 mL | 2.5285 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
