| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
IC50: 1.36 μM (URAT1-mediated 14C-UA uptake), 16.97 μM (CYP1A2), 5.22 μM (CYP2C9), >20 μM (CYP2C19), >20 μM (CYP2D6), and >20 μM (CYP3A4M)[1].
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|---|---|
| ln Vitro |
URAT1-mediated 14C-UA uptake (IC50 = 1.36 μM) and CYP cell activity are inhibited by URAT1 inhibitor 2 (compound 23) (0-50 μM, 3-20 min)[1].
|
| ln Vivo |
URAT1 inhibitor 2 (orally at 10 mg/kg or intravenously at 2 mg/kg) exhibits an oral bioavailability of 59.3% and favorable pharmacokinetic properties[1]. In acute hyperuricemia mice, oral URAT1 inhibitor 2 (4, 2, 1, 0.5, and 0.25 mg/kg; Orally) exhibits remarkable and potent SUA-lowering effect in a dose-dependent manner[1]. Favorable safety profiles and no discernible acute toxicity are shown by URAT1 inhibitor 2 (1000 mg/kg, intragastric injection, once)[1]. URAT1 inhibitor 2 pharmacokinetic parameters in male Sprague-Dawley rats[1]. parameters unit poiv compoundmax (h) 23 23 AUC (0-t) ng/mL·h 48754.6 16344.8 AUC (0-∞) ng/mL ·h 48781.5 16448.8 MRT (0-∞) h 3.3 1.0 t1/2 h 2.2 1.8 Tmax h 0.3 Cmax ng/mL 19185.0 CL mL/min/kg 2.2 F % 59.3
|
| Cell Assay |
Cell Viability Assay
Cell Types: Human URAT1, CYP cells[1] Tested Concentrations: 0, 0.05, 0.15, 0.5, 1.5, 5.0, 15, and 50 μM Incubation Duration: 3-20 min Experimental Results: Inhibited URAT1-mediated 14C-UA uptake and CYP cell activity. |
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (n=10)[1]
Doses: 2 mg/kg (intravenous) or 10 mg/kg (oral administration) Route of Administration: intravenous (iv) or oral administration Experimental Results: Achieved excellent pharmacokinetic/PK properties with the oral bioavailability of 59.3%. Animal/Disease Models: Acute hyperuricemia mice[1] Doses: 4, 2, 1, 0.5, and 0.25 mg/kg Route of Administration: Orally, once Experimental Results: demonstrated outstanding SUA-lowering activity. Animal/Disease Models: Kunming mice[1] Doses: 1000 mg/kg Route of Administration: Itragastric administration, once Experimental Results: demonstrated favorable safety profiles and no obvious acute toxicity. |
| References |
| CAS # |
2803951-18-8
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|---|---|
| Appearance |
Typically exists as solid at room temperature
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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)
|
| 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.) |
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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