| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
The metabolic stability of EP4 receptor antagonist 8 (Compound 27i) (100 μg/mL, 0–60 min) in rat liver microsomes (RLM) decreased over time, with a remaining percentage of 41.44% at 60 min [1]. EP4 receptor antagonist 8 (24 h) showed moderate plasma protein binding (97.60%) at 24 h [1]. EP4 receptor antagonist 8 significantly reduced IL-6 levels in lipopolysaccharide (LPS)-induced RAW 264.7 cells in a dose-dependent manner [1].
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|---|---|
| ln Vivo |
EP4 receptor antagonist 8 (compound 27i) (5-20 mg/kg, intraperitoneal injection, single injection, 24 hours after CFA injection, as per instructions) showed significant anti-inflammatory and analgesic effects in a Freund's adjuvant (CFA)-induced C57BL/6 joint inflammation model in a dose-dependent manner [1]. EP4 receptor antagonist 8 (5-20 mg/kg, simplest, once daily for 5 days) showed potent anti-inflammatory activity in a Kunming critical activation model [1].
|
| Cell Assay |
ELISA Assay[1]
Cell Types: Lipopolysaccharides (LPS)-induced RAW 264.7 cells Tested Concentrations: 6.25 μM, 12.5 μM, 25 μM, 50 μM Incubation Duration: Pretreated 1 h, then simulated with LPS for 24 h Experimental Results: Reduced LPS-induced IL-6 levels in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Chronic arthritis was induced in the right hind paw using C57BL/6 mice (female, weighing 20-22 g) by injection of complete Freund's adjuvant (CFA)[1].
Doses: 5 mg/kg, 10 mg/kg, 20 mg/kg Route of Administration: I.p., once, performed 24 hours after CFA injection Experimental Results: Significantly improved the swelling of mice paws in a dose-dependent manner. Increased the pain threshold; in both the hot plate test and the Von Frey test, the 20 mg/kg group showed the best effect within 120 minutes. Reduced joint inflammation, cartilage damage, bone erosion, and pannus formation. Reduced IL-1β, IL-6, and TNF-α positive cells in joint tissue. Animal/Disease Models: Acute ear inflammation and swelling were induced in male Kunming mice (weighing 20-22 g) by uniformly applying xylene (20 μL) to the right ear[1]. Doses: 5 mg/kg, 10 mg/kg, 20 mg/kg Route of Administration: P.o., once daily for 5 days Experimental Results: Showed excellent inhibitory effect, and the inhibitory rate was as high as 47.09 %, which was dose-dependent. |
| References |
| Molecular Formula |
C26H21CLN6O4
|
|---|---|
| Molecular Weight |
516.94
|
| CAS # |
3068255-86-4
|
| Appearance |
Typically exists as solids at room temperature
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| 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
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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 | 1.9345 mL | 9.6723 mL | 19.3446 mL | |
| 5 mM | 0.3869 mL | 1.9345 mL | 3.8689 mL | |
| 10 mM | 0.1934 mL | 0.9672 mL | 1.9345 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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