| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
URAT1 inhibitor 10 (5 μM; 30min) inhibits the activity of OAT1 in MDCK-hOAT cells (IC50 =9.17 μM)[1]. URAT1 inhibitor 10 (24 h) has a moderate inhibitory effect on IL-6 in RAW264.7 cells (IR = 25.6%), which may alleviate the symptoms associated with MSU crystal-mediated inflammatory cytokines[1]. URAT1 inhibitor 10 shows low cytotoxicity to HepG2 cells (IC50 > 64 μg/mL)[1].
|
|---|---|
| ln Vivo |
URAT1 inhibitor 10 (50 mg/kg; po) has good pharmacokinetic properties[1]. URAT1 inhibitor 10 (10 mg/kg; po once a day for seven days) showed a significant decrease in serum uric acid (SUA) in the hyperuricemia mouse model induced by potassium oxalate, with a reduction rate of 53.9%, which is equivalent to the positive control Lesinurad (HY-15258) at the same dose[1]. Pharmacokinetic Analysis in URAT1 inhibitor 10 Model[1]
|
| Animal Protocol |
Animal/Disease Models:hyperuricemia mice [1]
Doses: 10 mg/kg； Once a day for seven days Route of Administration: p.o. Experimental Results: Exhibited significant serum uric acid-lowering activity. The serum uric acid (SUA) levels decreased to 424 μM, achieving a reduction ratio of 53.9%. This performance was comparable to that of the positive control, Lesinurad (HY-15258), which also demonstrated significant SUA-lowering effects at the same dose. |
| References |
| Molecular Formula |
C19H20F3N3O3S
|
|---|---|
| Molecular Weight |
427.44
|
| CAS # |
3012586-38-5
|
| Appearance |
Typically exists as solid 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 | 2.3395 mL | 11.6975 mL | 23.3951 mL | |
| 5 mM | 0.4679 mL | 2.3395 mL | 4.6790 mL | |
| 10 mM | 0.2340 mL | 1.1698 mL | 2.3395 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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