| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CHF6333 (Compound 15) (1 μM, 0-30 min) xinafoate has a half-life (t1/2) greater than 240 min in both human and mouse liver microparticles [1]. CHF6333 (10 μM, 4 h) xinafoate has a binding rate of 60.0% to human plasma proteins and 58.0% to mouse plasma proteins [1]. After incubation for 1 hour in mouse or human lung S9 fractions, more than 80% of CHF6333 (1 μM, 1 h) xinafoate remains unmetabolized [1]. CHF6333 (0.014-10 μM) xinafoate has an IC50 value greater than 10 μM against all CYP450 isoenzymes (CYP1A1, CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4 and CYP3A5)[1]. CHF6333 xinafoate has an IC50 value of 24.7 μM against acetylcholinesterase[1]. CHF6333 xinafoate has an IC50 value greater than 100 μM against the M2 receptor and an IC50 value of 67.3 μM against the M3 receptor[1]. CHF6333 (100 μM) xinafoate does not inhibit hERG channels in HEK-293 cells and has no cardiovascular toxicity risk[1]. CHF6333 (1-100 μM, 24 hours) xinafoate showed no cytotoxicity to SAEC (human respiratory epithelial cells) and HepG2 (human liver cancer cells) at high concentrations, demonstrating its good safety [1].
|
|---|---|
| ln Vivo |
CHF6333 (0.03-0.6 mg/kg, tracheal spray, once) xinafoate can effectively prevent lung tissue damage directly caused by NE [1].
|
| Animal Protocol |
Animal/Disease Models: Sprague-Dawley (SD) rats were induced to have acute lung injury and pulmonary hemorrhage by direct intratracheal (intratracheal) injection of exogenous human neutrophil elastase (NE, 100 U/rat)[1].
Doses: 0.03 mg/kg, 0.3 mg/kg, 0.6 mg/kg Route of Administration: Intratracheal, once Experimental Results: Significantly reduced hemoglobin concentration in BALF (i.e., pulmonary hemorrhage) in a dose-dependent manner. |
| References |
| Molecular Formula |
C38H35F3N6O6
|
|---|---|
| Molecular Weight |
728.72
|
| CAS # |
3071964-44-5
|
| Related CAS # |
CHF-6333
|
| 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 | 1.3723 mL | 6.8613 mL | 13.7227 mL | |
| 5 mM | 0.2745 mL | 1.3723 mL | 2.7445 mL | |
| 10 mM | 0.1372 mL | 0.6861 mL | 1.3723 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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