878672-00-5
RDEA 594
CAS: 878672-00-5
Molecular Formula: C17H14BrN3O2S
878672-00-5 - Names and Identifiers
878672-00-5 - Physico-chemical Properties
| Molecular Formula | C17H14BrN3O2S |
| Molar Mass | 404.28 |
| Density | 1.72±0.1 g/cm3(Predicted) |
| Melting Point | >171oC (dec.) |
| Boling Point | 643.7±65.0 °C(Predicted) |
| Solubility | 25°C: DMSO |
| Appearance | Form Solid, color White to Off-White |
| pKa | 2.91±0.10(Predicted) |
| Storage Condition | -20°C Freezer, Under inert atmosphere |
| Physical and Chemical Properties | Bioactive Lesinurad (RDEA-594) is a selective uric acid reabsorption inhibitor. |
| Use | Application of Resinard is the first listed urate reuptake transporter inhibitor, which is combined with xanthine oxidase inhibitor to treat hyperuricemia associated with gout. |
878672-00-5 - Introduction
Lesinurad(RDEA594) is a URAT1 inhibitor that regulates uric acid secretion.
Last Update：2022-10-16 17:30:56
878672-00-5 - Uses and synthesis methods
Introduction
Resinard was approved by the U.S. Food and Drug Administration (FDA) on December 22, 2015, and then approved by the European Medicines Agency (EMA) on February 18, 2016. The compound was earlier developed by Ardea. AstraZeneca acquired the company in 2012, which in turn acquired the product. The drug's trade name is Zurampic® in the United States and the European Union. Lesinurad is the world's first approved urate reuptake transporter (URAT1) inhibitor, combined with xanthine oxidase inhibitors to treat hyperuricemia-related gout.
Pharmacological action
Resinard is an oral prostacyclin receptor (IP receptor) agonist, which is structurally different from prostacyclin. Resinard is hydrolyzed by carboxylesterase to produce its active metabolite, which is about 37 times more potent than Resinard's. Compared with other prostaglandin receptors (EP1-4,DP,FP, and TP), Resinard and the active metabolite are selective for IP receptors.
mechanism of action
Resinard (Lesinurad), trade name Zurampic. Recinard in combination with xanthine oxidase inhibitor (XOI) for hyperuricemic gout syndrome. On December 17, the European Union was approved by the European Union. Its mechanism of action is to help the kidneys excrete uric acid, and it works by inhibiting the function of transporters involved in uric acid reabsorption in the kidneys.
hyperuricemic drugs
on December 22, 2015, FDA approved the listing of a new hyperuricemia drug, Lesinurad, developed by AstraZeneca's Ardea Biosciences, with a trade name of Zurampic. Recinard in combination with xanthine oxidase inhibitor (XOI) for hyperuricemic gout syndrome. On December 17, the European Union was approved by the European Union. Its mechanism of action is to help the kidneys excrete uric acid, and it works by inhibiting the function of transporters involved in uric acid reabsorption in the kidneys.
Target
Target Value
URAT1
in vitro studies
Lesinurad inhibits the uric acid transport activity (IC50=3.36 μM) of hURAT1 (human URAT1), which is more than 20 times the inhibitory effect on rURAT1 (rat URAT1) (IC50=74.84 μM). Lesinurad inhibit hURAT1 through the interaction of the key amino acid residue Phe365.
Last Update：2024-04-10 22:29:15
878672-00-5 - Nature
| Solubility | DMSO (Slightly), Methanol (Slightly, Heated) |
Last Update：2024-04-10 22:29:15
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