| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CX116 (compound 83) (10 μM, 1 h) exhibited potent anti-inflammatory and cytoprotective effects, with an IC50 of 1.1 μM and an EC50 of 0.8 μM for NO inhibition in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells [1]. CX116 (1.25–10 μM, 10 μM cisplatin pretreatment, 1 h) inhibited the levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, and MCP-1) associated with cisplatin-induced acute kidney injury (cis-AKI) in cisplatin-induced HK-2 cells in a concentration-dependent manner [1]. CX116 (2.5–10 μM, 10 μM cisplatin pretreatment) reduced the levels of p-P65, COX-2, and iNOS proteins in a dose-dependent manner [1]. CX116 (2.5-10 μM, 10 μM cisplatin pretreatment) reduced ROS levels induced by 10 μM cisplatin in a dose-dependent manner [1]. CX116 (2.5-10 μM, 10 μM cisplatin pretreatment) had a significant protective effect on the structure and function of mitochondria in HK-2 cells [1]. CX116 (2.5-10 μM, 10 μM cisplatin pretreatment, 24 h) increased the expression levels of sirtuin3, Opa1 and ATP5A1 in a concentration-dependent manner. CX116 (2.5-10 μM, 10 μM cisplatin pretreatment) reduced the expression levels of P53, c-caspase 3 and Bax proteins and increased the expression of Bcl-2 protein, thereby attenuating cisplatin-induced apoptosis in HK-2 cells [1]. CX116 (2.5-10 μM, 10 μM cisplatin pretreatment) can significantly reduce the tailing phenomenon in the DNA head region and reduce the degree of DNA damage[1]. The IC50 values of CX116 (24 h) against five cytochrome P450 enzyme (CYP) isoforms were 26.8 μM (LA-2), 14.2 μM (2C9), 13.7 μM (2C19), 34.5 μM (2D6) and >50 (3A4)[1].
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|---|---|
| ln Vivo |
CX116 (compound 83) (1500 mg/kg, orally, single high dose) did not cause death, toxicity, or significant weight loss in C57BL/6 mice [1]. CX116 (25, 50 mg/kg, by gavage, once daily for 6 days) significantly reduced cisplatin-induced nephrotoxicity in mice and exerted a significant renal protective effect [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: HK-2 cells Tested Concentrations: 2.5, 5, 10 μM, 10 μM cisplatin pretreatment Incubation Duration: 24 hours Experimental Results: Cisplatin stimulation resulted in a dose-dependent decrease in P65 levels. COX-2 and IOS expression were inhibited in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models:Mouse model (6-8 week old male C57BL/6 mice, weighing 18-20 g), single intraperitoneal injection of 20 mg/kg cisplatin.
Doses: 25, 50 mg/kg. Route of Administration: Gavage (ig), once daily, from 3 days before to 3 days after cisplatin administration. Experimental Experimental Results: The kidneys of the high-dose group showed a more normal mouse appearance. It reduced renal cell damage and inflammatory cell infiltration, as evidenced by decreased BUN and SCR levels. The activity of the high-dose group was slightly superior to amifostine. It reduced the levels of pro-inflammatory factors TNF-α and IL-1β. It reduced the expression of KIM-1 and NGAL. |
| References |
| Molecular Formula |
C23H24N6O3
|
|---|---|
| Molecular Weight |
432.48
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
NC1=NC=C(C=C1C(NC2=CC=C(C=C2)NC(C)=O)=O)C3=CC=C(N=C3)N4CCOCC4
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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 | 2.3122 mL | 11.5612 mL | 23.1225 mL | |
| 5 mM | 0.4624 mL | 2.3122 mL | 4.6245 mL | |
| 10 mM | 0.2312 mL | 1.1561 mL | 2.3122 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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