| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
LY3023703 (compound 8) effectively inhibits human mPGES-1 microsomes with an IC50 value of 0.9 nM[1]. LY3023703 has a weak inhibitory effect on rat mPGES-1 microsomes with an IC50 value of 33.9 μM[1]. LY3023703 can inhibit the production of PGE2 in IL-1β-stimulated A549 cells with an IC50 value of 12 nM, but does not affect the production of PGI2[1]. LY3023703 can inhibit the production of PGE2 in human whole blood stimulated by LPS with an IC50 value of 12 nM and an IC80 value of 69 nM, but does not affect the production of TXB2 or PGF2α[1]. LY3023703 inhibits LPS-stimulated PGE2 production in canine whole blood with an IC50 of 139 nM and an IC80 of 703 nM[1]. LY3023703 (10 μM; pre-incubation for 30 min, reaction for 1 min) weakly inhibits microsomal CYP3A4 in a time-dependent manner[1]. LY3023703 has an IC50 of 82.6 μM for inhibiting hERG channels, while its IC80 for human whole blood PGE2 is 69 nM[1]. LY3023703 (compound 2) strongly inhibits mPGES-1-mediated PGE2 production in human whole blood with an IC50 of 0.012 μM[2].
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| References |
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| Molecular Formula |
C23H22F5N5O2
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|---|---|
| Molecular Weight |
495.45
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| CAS # |
1415089-24-5
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CC(CNC(C(C)C)=O)=CN=C1C(F)F)NC2=NC(C)=C(C3=CC=C(C(F)(F)F)C=C3)N2
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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 | 2.0184 mL | 10.0918 mL | 20.1837 mL | |
| 5 mM | 0.4037 mL | 2.0184 mL | 4.0367 mL | |
| 10 mM | 0.2018 mL | 1.0092 mL | 2.0184 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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