| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
GLUT9 18.21 μM (IC50)
|
|---|---|
| ln Vitro |
URAT1/GLUT9-IN-1 has the most potent inhibitory effect on urat1-mediated 14C-uric acid uptake (IC50= 2.01 μM), which is about three times that of Lesinurad (HY-15258) (IC50= 5.54 μM) [1]. The in vitro inhibitory activity of URAT1/GLUT9-IN-1 (5 μM) on GLUT9 is slightly better than that of Benzbromarone (HY-B1135), with an IC50 value of 18.21±1.03 μM [1]. The inhibition rate of URAT1/GLUT9-IN-1 (10 μM) on XOD is less than 20%, indicating that its inhibitory effect is negligible [1]. URAT1/GLUT9-IN-1 has an inhibitory potential to inhibit CYP (CYP2C9 (IC50= 2.00 μM) and CYP2C19 (IC50= 5.93 μM)) drug metabolizing enzymes, indicating low hepatotoxicity [1].
|
| ln Vivo |
The minimum effective dose of URAT1/GLUT9-IN-1 (0.25, 0.5, 1 mg/kg, po) in reducing SUA activity in mouse models of acute hyperuricemia is approximately 0.5 mg/kg [1]. URAT1/GLUT9-IN-1 (2mg/kg, po) shows great potential as a drug candidate to reduce SUA activity, being approximately 1.8-fold more potent than Lesinurad (HY-15258) in stable hyperuricemia in rat models [1]. URAT1/GLUT9-IN-1 (100 mg/kg, 100 mg/kg, orally administered every other day, for 14 days) is significantly safer than the Lesinurad (HY-15258) group in mice with chronic hyperuricemia[1] . Pharmacokinetic Analysis in SD rats[1] Route Dose (mg/kg) AUC0_t (ng·h/mL) AUC0_INF (ng·h/mL) MRT0_INF (h) T1/2 (h) Tmax (h) Cmax (ng/mL ) Cl (L·h/kg) F (%) po 2 1813.4 7929.1 2.5 1.8 0.25 1272.7 / 20.1 iv 2 1903.7 1922.9 0.5 1.6 0.083 6591.8 17.5 /
|
| Animal Protocol |
Animal/Disease Models:stable hyperuricemia rat model
Doses: 2 mg/kg Route of Administration: Oral gavage (p.o.) Experimental Results: Had 90.12% titer ratio of decreasing sua activity. |
| References |
| Molecular Formula |
C23H21N3O2S2
|
|---|---|
| Molecular Weight |
435.56
|
| CAS # |
2883011-18-3
|
| 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 | 2.2959 mL | 11.4795 mL | 22.9589 mL | |
| 5 mM | 0.4592 mL | 2.2959 mL | 4.5918 mL | |
| 10 mM | 0.2296 mL | 1.1479 mL | 2.2959 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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