Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
COX-2
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ln Vitro |
With an IC50 of 0.84 μM, >50 μM, and 0.60 μM, respectively, COX-2-IN-6 (Compound 10) inhibits the human COX-2/COX-1 enzyme and COX-2/COX-1-driven PGE2 synthesis in HEK293 cells. and greater than 50 μM[1]. In vitro, COX-2-IN-6 demonstrates stability in hepatocytes and human or mouse liver microsomes. Human hepatocytes have a T1/2 value of 3.1 minutes, while mouse hepatocytes have a T1/2 value of 3.0 minutes[1].
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ln Vivo |
In the APCmin/+ mouse model, COX-2-IN-6 (Compound 10) (30-300 mg/kg; oral; single dosage) slows the evolution of adenoma and increases survival[1]. With a C/P distribution ratio of more than 1200 in 4 hours, COX-2-IN-6 (10 mg/kg; oral; single dose) shows substantial colonic exposure (>4300 ng/g) and minimal systemic exposure (<6 ng/mL)[1].
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Animal Protocol |
Animal/Disease Models: APCmin/+ mouse model[1]
Doses: 30 mg/kg, 100 mg/kg, 300 mg/kg Route of Administration: PO; daily in chow diet Experimental Results: Dramatically diminished [18F]-FDG uptake and polyp area. |
References |
[1]. Zhang Z, et al. Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer. J Med Chem. 2021 Aug 12;64(15):11570-11596.
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Molecular Formula |
C20H27NO6S
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Molecular Weight |
409.50
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CAS # |
2756347-91-6
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SMILES |
C1(OCCC)=NC(OCC(O)(C)C)=C(C2=CC=C(S(C)(=O)=O)C=C2)C=C1CO
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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) |
DMSO: 100 mg/mL (244.20 mM)
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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 | 2.4420 mL | 12.2100 mL | 24.4200 mL | |
5 mM | 0.4884 mL | 2.4420 mL | 4.8840 mL | |
10 mM | 0.2442 mL | 1.2210 mL | 2.4420 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.