| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
The target is URAT1 (SLC22A12). Xininurad inhibits URAT1-mediated urate reabsorption in the proximal tubule, increasing urinary urate excretion and lowering serum uric acid. Its potency is substantially greater than that of earlier URAT1 inhibitors such as benzbromarone and lesinurad.
|
|---|---|
| ln Vitro |
Xininurad inhibits human URAT1 with IC50 = 7.17 nM, more than 40-fold lower than benzbromarone and lesinurad. It is orally active and produces dose-dependent reductions in serum urate in preclinical models, with a favorable potency profile for clinical development.
|
| ln Vivo |
In clinical studies, xininurad lowers serum uric acid in patients with hyperuricemia and gout. Preclinical in vivo data show dose-dependent urate-lowering activity after oral administration, consistent with URAT1 inhibition in the kidney.
|
| Enzyme Assay |
URAT1 inhibition is measured using URAT1-expressing HEK293 cells and radiolabeled or fluorescent urate; the compound is titrated, and IC50 values are derived from the inhibition of urate uptake. Selectivity is assessed against other urate transporters (e.g., GLUT9, OAT1, OAT3).
|
| Cell Assay |
URAT1-expressing cells are incubated with the compound and a labeled urate substrate; intracellular urate accumulation is quantified by scintillation counting or fluorescence. Cytotoxicity is assessed in parallel to distinguish transporter inhibition from nonspecific effects.
|
| Animal Protocol |
Rodents or humans receive xininurad orally; serum urate and urinary urate excretion are measured serially, and pharmacokinetic parameters are determined by LC-MS/MS. In clinical trials, dose-response urate-lowering efficacy and safety are assessed in hyperuricemic patients.
|
| References |
| Molecular Formula |
C15H10BR2FN3O2
|
|---|---|
| Molecular Weight |
443.065205097198
|
| Exact Mass |
442.91
|
| CAS # |
2365178-28-3
|
| PubChem CID |
139329673
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
4.7
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
446
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(C1=CC(Br)=C(O)C(Br)=C1)(C1N2C(=NC=1CC)N=CC(F)=C2)=O
|
| InChi Key |
ACXPMDYWZAUOJS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H10Br2FN3O2/c1-2-11-12(21-6-8(18)5-19-15(21)20-11)13(22)7-3-9(16)14(23)10(17)4-7/h3-6,23H,2H2,1H3
|
| Chemical Name |
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-6-fluoroimidazo[1,2-a]pyrimidin-3-yl)methanone
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~50 mg/mL (~112.85 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.64 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 25.0 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 | 2.2570 mL | 11.2849 mL | 22.5698 mL | |
| 5 mM | 0.4514 mL | 2.2570 mL | 4.5140 mL | |
| 10 mM | 0.2257 mL | 1.1285 mL | 2.2570 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
