| ln Vitro |
HYJ-2 (10-10000 nM) effectively inhibited URAT1-mediated uric acid uptake in HEK293 cells overexpressing URAT1, with an IC50 value of 368 nM[1]. HYJ-2 showed low cytotoxicity to HEK293T cells, with an IC50 value of 353.1 μM[1]. HYJ-2 also showed low cytotoxicity to HepG2 cells, with an IC50 value of 287.3 μM[1]. HYJ-2 (100 μM; 24 h) did not significantly promote apoptosis in HepG2 cells[1]. HYJ-2 (100 μM; 24 h) had a weak effect on mitochondrial function in HepG2 cells, with 73.7% of the cells still maintaining a high mitochondrial membrane potential[1]. HYJ-2 exhibits excellent metabolic stability in human liver microsomes, with a half-life of 990 minutes and 97.3% of the parent drug residue remaining after 60 minutes of incubation [1].
|
|---|---|
| ln Vivo |
HYJ-2 (2 mg/kg; 19 days) reduced serum uric acid levels in male Kunming mice with hyperuricemia by 36.7%, while alleviating hyperuricemia-related kidney damage and without causing significant liver damage [1].
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: Human hepatocellular carcinoma HepG2 cells Tested Concentrations: 100 μM Incubation Duration: 24 hours Experimental Results: 5.6% apoptosis rate was induced in HepG2 cells, which was comparable to the control group. |
| Animal Protocol |
Animal/Disease Models:Kunming hyperuricemia mice (male, 19-21 g) [1]
Doses: 2 mg/kg Route of Administration: 19 days Experimental Results: The mean serum uric acid level decreased from 1042.3 μM to 683.3 μM, a reduction of 36.7%. It alleviated the renal pathological damage associated with long-term hyperuricemia. Compared with the control drug group, the renal tubular structure was better preserved and the infiltration of interstitial inflammatory cells was significantly reduced. No obvious liver pathological abnormalities were observed. |
| References |
| Molecular Formula |
C14H9CL2N3O2
|
|---|---|
| Molecular Weight |
322.15
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CC1=CC=CC2=C(C(C3=CC(Cl)=C(O)C(Cl)=C3)=O)N=NN21
|
| 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 | 3.1041 mL | 15.5207 mL | 31.0414 mL | |
| 5 mM | 0.6208 mL | 3.1041 mL | 6.2083 mL | |
| 10 mM | 0.3104 mL | 1.5521 mL | 3.1041 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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