LesinuradURAT1 inhibitor CAS# 878672-00-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 878672-00-5 | SDF | Download SDF |
| PubChem ID | 53465279 | Appearance | Powder |
| Formula | C17H14BrN3O2S | M.Wt | 404.28 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | RDEA594 | ||
| Solubility | DMSO : ≥ 100 mg/mL (247.35 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-1,2,4-triazol-3-yl]sulfanyl]acetic acid | ||
| SMILES | C1CC1C2=CC=C(C3=CC=CC=C23)N4C(=NN=C4Br)SCC(=O)O | ||
| Standard InChIKey | FGQFOYHRJSUHMR-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H14BrN3O2S/c18-16-19-20-17(24-9-15(22)23)21(16)14-8-7-11(10-5-6-10)12-3-1-2-4-13(12)14/h1-4,7-8,10H,5-6,9H2,(H,22,23) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.In Vitro:Lesinurad is a novel selective uric acid reabsorption inhibitor (SURI). Lesinurad is determined to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with Km values of 0.85 and 2 µM, respectively[1]. Lesinurad (RDEA594) is a URAT1 and OAT inhibitor, which increases proximal renal tubule urate excretion[2]. Lesinurad (RDEA594) is a potential uric acid lowering agent througn inhibition of uric acid reuptake, and exhibits favorable p450 profiles, inhibits CYP2C9 and CYP2C8 with IC50 of 14.4 μM and 16.2 μM, respectively. IC50s of Lesinurad are all above 100 µM for CYP1A2, CYP2C19,and CYP2D6[3].In Vivo:Lesinurad (RDEA594) shows better pharmacokinetics than its pro-drug RDEA806. The 100 mg dose of Lesinurad exhibits a phamacological effect in the range of that produced by 300 mg to 800 mg single doses of RDEA806[3]. References: | |||||
Lesinurad Dilution Calculator
Lesinurad Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4735 mL | 12.3677 mL | 24.7353 mL | 49.4707 mL | 61.8383 mL |
| 5 mM | 0.4947 mL | 2.4735 mL | 4.9471 mL | 9.8941 mL | 12.3677 mL |
| 10 mM | 0.2474 mL | 1.2368 mL | 2.4735 mL | 4.9471 mL | 6.1838 mL |
| 50 mM | 0.0495 mL | 0.2474 mL | 0.4947 mL | 0.9894 mL | 1.2368 mL |
| 100 mM | 0.0247 mL | 0.1237 mL | 0.2474 mL | 0.4947 mL | 0.6184 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Lesinurad is an inhibitor of URAT1 that promoting renal uric acid excretion [1].URAT1 is a transporter in the kidney that regulates uric acid excretion from the body [2].
In the clinical study, lesinurad potently inhibit URAT1 as well as OAT4, another transporter responsible for the renal resorption of urate. In a study, 21 people with hyperuricemia or gout (sUA >= 8.0 mg/dL) were randomized to lesinurad, open-label allopurinol or placebo. Most of the lesinurad-treated patients had sUA < 6 mg/dL after seven days, which were the same effect to patients receiving allopurinol and better than placebo. Also, Lesinurad showed well tolerated in the study [2]. Compared with probenecid, whose efficacy is reducing patients with renal insufficiency, lesinurad may be effective in patients with mildly impaired renal function [1].
References:
[1]. Crittenden DB, Pillinger MH. New therapies for gout. Annu Rev Med, 2013, 64: 325-337.
[2]. Singh JA. Emerging therapies for gout. Expert Opin Emerg Drugs, 2012, 17(4): 511-518.
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Discovery and Assessment of Atropisomers of (+/-)-Lesinurad.[Pubmed:28337320]
ACS Med Chem Lett. 2017 Feb 14;8(3):299-303.
(+)- and (-)-Lesinurad were isolated as atropisomers from racemic Lesinurad for the first time. No interconversion was observed between the two atropisomers under various conditions tested. The two atropisomers showed significant differences in hURAT1 highly expressed HEK293 cell-based inhibition assays, monkey pharmacokinetic studies, and in vitro human recombinant CYP2C9 stability studies. It was speculated that (+)-Lesinurad might offer a better hyperuricemia/gout therapy than (-)-Lesinurad or the racemate.
Evaluation of Pharmacokinetic Interactions Between Lesinurad, a New Selective Urate Reabsorption Inhibitor, and Commonly Used Drugs for Gout Treatment.[Pubmed:28074640]
Clin Pharmacol Drug Dev. 2017 Jul;6(4):377-387.
Lesinurad is a novel selective uric acid reabsorption inhibitor approved for treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors (XOIs). Open-label pharmacokinetic studies were performed in volunteers or subjects with hyperuricemia (serum uric acid >/= 8 mg/dL) to investigate interactions of Lesinurad (with and without concurrent XOIs) with colchicine and 2 nonsteroidal anti-inflammatory drugs: naproxen and indomethacin. Colchicine studies included consecutive 7-day treatment periods of (1) allopurinol 300 mg, allopurinol 300 mg plus Lesinurad 400 or 600 mg, and continued Lesinurad 400 or 600 mg; or (2) febuxostat 40 or 80 mg, febuxostat 40 or 80 mg plus Lesinurad 400 mg, and continued febuxostat 40 or 80 mg plus Lesinurad 600 mg. Naproxen and indomethacin studies included Lesinurad 400 mg on day 1, naproxen 250 mg twice daily or indomethacin 25 mg twice daily on days 2-6, and Lesinurad 400 mg plus continued naproxen or indomethacin on days 7-13 and the morning of day 14. Lesinurad did not alter the pharmacokinetics of naproxen and modestly altered exposure to colchicine (AUC decrease of Lesinurad, whereas naproxen modestly decreased the Cmax of Lesinurad by approximately 27%.
Lesinurad: A significant advancement or just another addition to existing therapies of gout?[Pubmed:28163535]
J Pharmacol Pharmacother. 2016 Oct-Dec;7(4):155-158.
Gout is a metabolic disorder that usually presents as recurrent episodes of acute arthritis due to deposition of crystals in joints and cartilages. Despite the availability of several drugs for gout, its management is still less than adequate. There is always a search for newer, safer, and more potent urate-lowering therapies for treating patients inadequately controlled with available drugs. Lesinurad in combination with a xanthine oxidase inhibitor provides an effective mode of therapy in the management of hyperuricemia associated with gout. Lesinurad is a selective uric acid transporter 1 (URAT1) inhibitor. URAT1 is responsible for the majority of uric acid absorption from kidneys to the circulation. Lesinurad was granted marketing approval based on three randomized, double-blind, placebo-controlled; phase III clinical trials. It is devoid of interaction with organic anion transporters (OATs) such as OAT1 and 3, responsible for drug-drug interactions, an undesirable property associated with probenecid. On-going research is more focused on reducing inflammation consequent to deposition of crystals rather than production and excretion of urate. Various targets are being explored, and interleukin-1 beta inhibition seems to be one of the most promising approaches.
Evaluation of Pharmacokinetic Interactions Between Lesinurad, a New Selective Urate Reabsorption Inhibitor, and CYP Enzyme Substrates Sildenafil, Amlodipine, Tolbutamide, and Repaglinide.[Pubmed:28067999]
Clin Pharmacol Drug Dev. 2017 Jul;6(4):363-376.
Lesinurad is a selective uric acid reabsorption inhibitor approved for the treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors. In vitro assays indicate that Lesinurad is an inducer of CYPs in the order CYP3A > CYP2C8 > CYP2C9 > CYP2C19 > CYP2B6 and an inhibitor of CYP2C8 and CYP2C9. To investigate the drug interaction potential of Lesinurad, clinical drug interaction studies were conducted. Open-label studies in volunteers investigated the effects of single-/multiple-dose Lesinurad on the pharmacokinetics of sildenafil and amlodipine (CYP3A4 induction), tolbutamide (CYP2C9 inhibition/induction), and repaglinide (CYP2C8 inhibition/induction). There was no apparent induction of CYP2C8 and CYP2C9 following repeated Lesinurad administration, although no inhibition of CYP2C9 and modest inhibition of CYP2C8 were observed following single-dose Lesinurad. Consistent with in vitro observations, Lesinurad (200 mg once daily) was an inducer of CYP3A based on the effects on sildenafil exposure. Sildenafil exposure decreased by approximately 34% for Cmax and AUC when administered with multiple-dose Lesinurad 200 mg and allopurinol 300 mg, relative to sildenafil alone. During Lesinurad therapy, the possibility of reduced efficacy of concomitant drugs that are CYP3A substrates should be considered and their efficacy monitored because of induction of CYP3A by Lesinurad.
