| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CGS 23885 (compound 43) effectively inhibited the activity of 5-lipoxygenase in guinea pig polymorphonuclear leukocytes (PMNs), with an IC50 value of 43 nM for inhibiting 5-HETE production and 48 nM for inhibiting LTB4 production [1]. CGS 23885 showed a weak inhibitory effect on cyclooxygenase in the seminal vesicles of rams, with an IC50 value of 36 μM, and exhibited high selectivity for 5-lipoxygenase [1]. CGS 23885 showed a moderate inhibitory effect on human platelet 12-lipoxygenase, with an IC50 value of 0.64 μM [1]. CGS 23885 showed an IC50 value of 0.11 μM for inhibiting the activity of 5-lipoxygenase in canine whole blood [1]. CGS 23885 inhibited the activity of 5-lipoxygenase in human whole blood, with an IC50 value of 0.89 μM [1].
|
|---|---|
| ln Vivo |
CGS 23885 (1-30 mg/kg; orally; administered 1 hour before carrageenan injection and 1 hour before A23187 injection) inhibited A23187-induced biosynthesis of LTB4 and LTC4/D4/E4 in a rat pleurisy model in a dose-dependent manner, and the drug concentration in the pleural effusion was strongly positively correlated with the inhibitory effect on LTB4 (IC50 = 21 ng/mL) [2].
|
| Animal Protocol |
Animal/Disease Models:Sprague-Dawley rats (male, 220-235 g, pleurisy induced by intrapleural injection of κ-carrageenan and calcium ion carrier A23187) [2]
Doses: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg Route of Administration: Oral; 1 hour before carrageenan injection and 1 hour before A23187 injection Experimental Results: At a dose of 1 mg/kg, A23187 inhibited LTB4 biosynthesis by 32% and LTC4/D4/E4 biosynthesis by 4%. At a dose of 3 mg/kg, A23187 inhibited 73% of LTB4 biosynthesis and 33-35% of LTC4/D4/E4 biosynthesis. At a dose of 10 mg/kg, A23187 inhibited 93% of LTB4 biosynthesis and 52-67% of LTC4/D4/E4 biosynthesis. At a dose of 30 mg/kg, A23187 inhibited 97% of LTB4 biosynthesis and resulted in a significant 24% reduction in total cell influx. Pleural effusion concentration was positively correlated with the inhibition rate of LTB4 biosynthesis, with an IC50 of 21 ng/mL for LTB4 inhibition. At all doses, A23187 did not significantly affect exudate volume, PGE2 level, or TXB2 level; at doses of 1, 3, and 10 mg/kg, A23187 also did not significantly affect total cell influx. |
| References |
|
| Molecular Formula |
C17H16N2O4
|
|---|---|
| Molecular Weight |
312.32
|
| CAS # |
134822-78-9
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(N(CC1=CC2=C(OC1)C=CC(OC3=CC=CC=C3)=C2)O)N
|
| 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 | 3.2018 mL | 16.0092 mL | 32.0184 mL | |
| 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | |
| 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 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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