| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
IC50: 0.8 nM (URAT1)[1]
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| ln Vitro |
At high concentrations, URAT1 inhibitor 3 (0-400 μM; 24 and 72 h; HepG2 and HK2 cells) decreases cell viability with minimal toxicity[1]. The urate excretion transporters are less inhibited by URAT1 inhibitor 3 (0.01-100 μM), with IC50 values of 4.04 μM for ABCG2 and 10.16 μM for OAT1[1].
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| ln Vivo |
In a mouse model of hyperuricemia, URAT1 inhibitor 3 (1-4 mg/kg; ig; once) has the efficacy to decrease urate[1]. In mice, URAT1 inhibitor 3 (50 mg/kg; ig; daily, for 14 d) had no adverse effects on the liver or kidneys[1]. Kunming mice with a hyperuricemia model are subjected to GSH depletion induced by URAT1 inhibitor 3 (50 mg/kg; ig; once).
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HepG2 and HK2 cells Tested Concentrations: 0, 100, 200, 300, and 400 μM Incubation Duration: 24 and 72 hrs (hours) Experimental Results: Had little cytotoxicity at 24 h and inhibition rate of 34.75% and 35.9% of HepG2 and HK2 cells, respectively. |
| Animal Protocol |
Animal/Disease Models: Male Kunming (KM) mice with hyperuricemia model[1]
Doses: 1, 2, and 4 mg/kg Route of Administration: Oral gavage; once Experimental Results: diminished the serum urate levels in a dose-dependent manner. Animal/Disease Models: Male Kunming mice[1] Doses: 50 mg/kg Route of Administration: Oral gavage; daily, for 14 days Experimental Results: Did not cause renal toxicity. Animal/Disease Models: Male Kunming mice with hyperuricemia model[1] Doses: 50 mg/kg Route of Administration: Oral gavage; once Experimental Results: diminished the serum GSH levels from 42.23 μM to 20.39 μM. |
| References |
[1]. Zhao Z, et, al. Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents. Eur J Med Chem. 2022 Nov 15;242:114682.
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| Molecular Formula |
C14H8CL2N2O2
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|---|---|
| Molecular Weight |
307.13
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| CAS # |
2850331-30-3
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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)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (325.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 10 mg/mL (32.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2560 mL | 16.2798 mL | 32.5595 mL | |
| 5 mM | 0.6512 mL | 3.2560 mL | 6.5119 mL | |
| 10 mM | 0.3256 mL | 1.6280 mL | 3.2560 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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