[CAS NO. 1151516-14-1] Lesinuradsodium
PRODUCTS SPECIFICATIONS [1151516-14-1]
DESCRIPTION [1151516-14-1]
Overview
| MDL | MFCD24444603 |
|---|---|
| Molecular Weight | 426.26 |
| Molecular Formula | C17H13BrN3NaO2S |
| SMILES | O=C(O[Na])CSC1=NN=C(Br)N1C2=C3C=CC=CC3=C(C4CC4)C=C2 |
1 Publications Citing Use of MCE
Summary
Lesinurad sodium is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K m values of 0.85 and 2 µM, respectively.
IC50 & Target
Km: 0.85 µM (OAT1), 2 µM (OAT3) [1]
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 K m 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 IC 50 of 14.4 μM and 16.2 μM, respectively. IC 50 s of Lesinurad are all above 100 µM for CYP1A2, CYP2C19,and CYP2D6 [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01493531 | Ardea Biosciences, Inc. |
Gout
|
December 2011 | Phase 3 |
| NCT01986556 | Ardea Biosciences, Inc. |
Healthy
|
November 2013 | Phase 1 |
| NCT02127775 | Ardea Biosciences, Inc. |
Healthy
|
April 2014 | Phase 1 |
| NCT02581553 | Ardea Biosciences, Inc. |
Healthy
|
October 2015 | Phase 1 |
| NCT01982201 | Ardea Biosciences, Inc. |
Healthy
|
November 2013 | Phase 1 |
| NCT01808131 | Ardea Biosciences, Inc. |
Gout
|
February 2013 | Phase 3 |
| NCT01508702 | Ardea Biosciences, Inc. |
Gout
|
January 2012 | Phase 3 |
| NCT03226899 | Ironwood Pharmaceuticals, Inc.|Medpace, Inc. |
Gout|Chronic Kidney Disease (CKD)
|
July 19, 2017 | Phase 4 |
| NCT01908257 | Ardea Biosciences, Inc. |
Healthy
|
July 2013 | Phase 1 |
| NCT01510769 | Ardea Biosciences, Inc. |
Tophaceous Gout
|
January 2012 | Phase 3 |
| NCT02039700 | Ardea Biosciences, Inc. |
Healthy
|
January 2014 | Phase 1 |
| NCT02888054 | Ardea Biosciences, Inc. |
Healthy
|
August 30, 2016 | Phase 1 |
| NCT02028689 | Ardea Biosciences, Inc. |
Healthy
|
October 2013 | Phase 1 |
| NCT01884272 | Ardea Biosciences, Inc. |
Gout
|
June 2013 | Phase 1 |
| NCT01510158 | Ardea Biosciences, Inc. |
Gout
|
January 2012 | Phase 3 |
| NCT03272425 | Ardea Biosciences, Inc. |
Gout
|
August 14, 2017 | Phase 1 |
| NCT01001338 | Ardea Biosciences, Inc. |
Gout
|
October 2009 | Phase 2 |
| NCT01650246 | Ardea Biosciences, Inc. |
Gout
|
August 2012 | Phase 3 |
| NCT00955981 | Ardea Biosciences, Inc. |
Hyperuricemia
|
July 2009 | Phase 2 |
| NCT01744379 | Ardea Biosciences, Inc. |
Gout
|
December 2012 | Phase 1 |
| NCT01808144 | Ardea Biosciences, Inc. |
Gout
|
March 1, 2013 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL ( 234.60 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3460 mL | 11.7299 mL | 23.4599 mL |
| 5 mM | 0.4692 mL | 2.3460 mL | 4.6920 mL |
| 10 mM | 0.2346 mL | 1.1730 mL | 2.3460 mL |
References
- [1] Shen Z, et al. In Vitro and In Vivo Interaction Studies Between Lesinurad, a Selective Urate Reabsorption Inhibitor, and Major Liver or Kidney Transporters. Clin Drug Investig. 2016 Jun;36(6):443-52
- [2] Sattui SE, et al. Treatment of hyperuricemia in gout: current therapeutic options, latest developments and clinical implications. Ther Adv Musculoskelet Dis. 2016 Aug;8(4):145-59.
- [3] L.Yeh, et al. RDEA594, a potential uric acid lowering agent througn inhibition of uric acid reuptake ,shows better pharmacokinetics rhan its prodrug RDEA806. 2008 ACR/ARHP Annual Scientific Meeting, 24-29 October 2008, USA.