1352792-74-5
Verinurad
CAS: 1352792-74-5
Molecular Formula: C20H16N2O2S
1352792-74-5 - Names and Identifiers
1352792-74-5 - Physico-chemical Properties
| Molecular Formula | C20H16N2O2S |
| Molar Mass | 348.42 |
| Density | 1.34±0.1 g/cm3(Predicted) |
| Melting Point | 204 - 207°C |
| Boling Point | 566.7±50.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| Appearance | Solid |
| Color | Off-White to Pale Brown |
| pKa | 2.91±0.10(Predicted) |
| Storage Condition | -20°C Freezer, Under inert atmosphere |
| In vitro study | Verinurad inhibited the transport activity of human URAT1 in a concentration-dependent manner with an IC50 of 25 nM. Verinurad also inhibited URAT1 related homologs OAT4 and OAT1 with IC50 of 5.9 μm and 4.6 μm, respectively, with 200-fold lower affinity than URAT. Verinurad had a 1640-fold higher affinity for human URAT1 than for rat URAT1 (human URAT1 IC50 = 0.025 μm, rat URAT IC50 = 41 μm). Verinurad is highly potent against human URAT1, and residues 35, 365 and 481 of URAT1 contribute to verinurad binding. A chimeric point mutation was introduced at position 365 of human URAT1 (phenylalanine at position 365 of human origin was replaced with tyrosine at position 365 of rat; h-F365Y), and the IC50 of verinurad was 4 μm, it was 160 times lower than that of wild type human-derived URAT1D. At the same time, if a similar point mutation is introduced into the input URAT1 (that is, tyrosine at position 365 of rats is mutated to phenylalanine at position 365 of human origin; r-Y365F),verinurad has an IC50 of 2.9 μm, than wild-type rat URAT1 14 times higher. |
| In vivo study | In the human body, Verinurad single drug is absorbed quickly, and its exposure (Cmax and ACC) increases with the increase of dose. In the starved state, the Cmax is reached 0.5-0.75 hours after administration; In the Fed state, the Cmax is reached 1.25 hours after administration. At different doses, t 1/2 is about 10-15 hours. Verinurad is well tolerated in vivo. In the systemic circulation, verinurad has a high clearance rate (CL/F ranging ~ 30-50 L/h) and is widely distributed extravascularly. Its renal excretion rate is low, only 2%-3% in the urine. Most of the verinurad may form metabolites in the liver by biotransformation. |
1352792-74-5 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.87 ml | 14.351 ml | 28.701 ml |
| 5 mM | 0.574 ml | 2.87 ml | 5.74 ml |
| 10 mM | 0.287 ml | 1.435 ml | 2.87 ml |
| 5 mM | 0.057 ml | 0.287 ml | 0.574 ml |
Last Update：2024-01-02 23:10:35
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Product Name: Verinurad Visit Supplier Webpage Request for quotationCAS: 1352792-74-5
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Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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