| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
sEH/FLAP-IN-2 (Compound 6) showed no significant inhibitory activity against 5-LOX, with an IC50 value >10 μM[1]. In human neutrophils, sEH/FLAP-IN-2 (10 μM, 15 min) significantly inhibited the production of 5-LOX products (LTB4, trans-LTB4 and 5-HETE) in the FLAP-dependent system in the absence of exogenous arachidonic acid (AA), with a residual activity of 35.7%; its inhibitory activity was weakened in the presence of exogenous AA (IC50 > 10 μM)[1]. sEH/FLAP-IN-2 (0.1-10 μM, 16 min) had no significant effect on the activities of COX-1, COX-2 and mPGES-1[1]. sEH/FLAP-IN-2 (0.1–10 μM, 120 min) inhibited 5-LOX/FLAP-derived mediators (such as LTB4 and LTC4) in a concentration-dependent manner, especially in M1-MDM; at the same time, it increased COX-derived prostaglandins (such as PGE2 and PGD2) but did not affect the level of SPM (such as RvD5)[1].
|
|---|---|
| ln Vivo |
sEH/FLAP-IN-2 (Compound 6) (10 mg/kg, intraperitoneal injection, once) effectively modulates the dialysis media spectrum in a rat peritonitis model by dual inhibition of FLAP and sEH, changing the dialysis media spectrum from a pro-inflammatory state (LTs and DHETs) to an anti-inflammatory state (EETs) [1].
|
| Animal Protocol |
Animal/Disease Models: CD-1 mice (33-39 g, 8 weeks old) were given an acute inflammatory response via intraperitoneal injection of Zymosan (1 mg/mouse)[1].
Doses: 10 mg/kg Route of Administration: I.p., once, 30 mins before zymosan Experimental Results: Significantly reduced zymosan-induced levels of pro-inflammatory mediators, including LTB4, 5-HETE, and LTE4. Increased levels of anti-inflammatory EETs (particularly 11,12-EET and 14,15-EET) while decreasing levels of pro-inflammatory DHETs (such as 11,12-DHET), resulting in an elevated EET/DHET ratio. PGE2 levels were significantly reduced, but TXB2 was unaffected. |
| References |
| Molecular Formula |
C26H33N5O2
|
|---|---|
| Molecular Weight |
447.57
|
| 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 | 2.2343 mL | 11.1714 mL | 22.3429 mL | |
| 5 mM | 0.4469 mL | 2.2343 mL | 4.4686 mL | |
| 10 mM | 0.2234 mL | 1.1171 mL | 2.2343 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
