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NLRP3/URAT1-IN-1 is an orally active dual inhibitor targeting NLRP3 and URAT1, with an IC50 of 3.81 μM. It suppresses IL-1β release in mouse bone marrow-derived macrophages (BMDMs) stimulated by LPS and ATP, with an IC50 of 2.61 μM. Additionally, NLRP3/URAT1-IN-1 decreases serum uric acid (SUA) levels and alleviates liver/kidney injury in mice with acute hyperuricemia (HUA). This compound is relevant for research on gout and hyperuricemia.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | NLRP3/URAT1-IN-1 is an orally active dual inhibitor targeting NLRP3 and URAT1, with an IC50 of 3.81 μM. It suppresses IL-1β release in mouse bone marrow-derived macrophages (BMDMs) stimulated by LPS and ATP, with an IC50 of 2.61 μM. Additionally, NLRP3/URAT1-IN-1 decreases serum uric acid (SUA) levels and alleviates liver/kidney injury in mice with acute hyperuricemia (HUA). This compound is relevant for research on gout and hyperuricemia. |
| Targets&IC50 | IL-1β:2.61 μM |
| In vitro | NLRP3/URAT1-IN-1 (Compound 32) demonstrates potent inhibitory activity against URAT1 in HEK293 cells overexpressing URAT1 with an IC50 value of 3.81 μM. It also inhibits OAT4 in HEK293-OAT4 cells using 6-carboxyfluorescein (6-CFL) as a substrate with an IC50 of 6.08 μM. In HEK293-GLUT9 cells overexpressing GLUT9, NLRP3/URAT1-IN-1 shows inhibitory effects with an IC50 of 11.02 μM, determined by whole-cell patch-clamp recording. Furthermore, at a concentration of 3 μM for 45 minutes, it reduces IL-1β release in LPS and ATP-stimulated mouse bone marrow-derived macrophages (BMDMs) with an IC50 of 2.61 μM, without affecting the production of TNF-α and IL-6. In human liver microsomes, it exhibits moderate inhibition of CYP2C9 (IC50 = 2.77 μM) and CYP2C19 (IC50 = 2.03 μM). |
| In vivo | NLRP3/URAT1-IN-1 (Compound 32) at a dose of 2 mg/kg, administered orally as a single dose, significantly reduces serum uric acid (SUA) levels in mice with acute hyperuricemia (HUA) induced by hypoxanthine and potassium oxonate. Moreover, a daily oral dose of 2 mg/kg for 3 days significantly alleviates ankle swelling in rats with acute gouty arthritis induced by intra-articular injection of MSU crystals. |
| Molecular Weight | 525.44 |
| Formula | C24H17BrN2O3S2 |
| Cas No. | 2994637-53-3 |
| Smiles | O=C(NS(=O)(=O)C=1SC=CC1)C2=CC=3C=CC=CC3N2CC4=CC=C(Br)C=5C=CC=CC54 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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