NLRP3/URAT1-IN-1
NLRP3/URAT1-IN-1 is an orally active double inhibitor of NLRP3 and URAT1 (IC50 = 3.81 μM). NLRP3/URAT1-IN-1 inhibits IL-1β release in LPS (HY-D1056) and ATP-stimulated mouse bone marrow-derived macrophages (BMDMs), with an IC50 of 2.61 μM. NLRP3/URAT1-IN-1 reduces serum uric acid (SUA) and alleviates liver/kidney damage in mice with acute hyperuricemia (HUA). NLRP3/URAT1-IN-1can be used for the study of gout and hyperuricemia.
For research use only. We do not sell to patients.
- CAS No.: 2994637-53-3
- Formula: C24H17BrN2O3S2
- Molecular Weight:525.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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IL-1β 2.61 μM (IC50) |
NLRP3 |
OAT4 6.08 μM (IC50) |
URAT1 3.81 μM (IC50) |
GLUT9 11.02 μM (IC50) |
NLRP3/URAT1-IN-1 (Compound 32) exhibits potent inhibitory activity against URAT1 in HEK293-URAT1-overexpressing cells, with an IC50 of 3.81 μM[1].
NLRP3/URAT1-IN-1 shows inhibitory effect on OAT4 in HEK293-OAT4-overexpressing cells using 6-carboxyfluorescein (6-CFL) as substrate, with an IC50 of 6.08 μM[1].
NLRP3/URAT1-IN-1 exerts inhibitory activity on GLUT9 in HEK293-GLUT9-overexpressing cells via whole-cell patch-clamp recordings, with an IC50 of 11.02 μM[1].
NLRP3/URAT1-IN-1 (3 μM, 45 min) inhibits IL-1β release in LPS (HY-D1056) and ATP-stimulated mouse bone marrow-derived macrophages (BMDMs), with an IC50 of 2.61 μM, and does not affect TNF-α and IL-6 production[1].
exhibits moderate inhibitory activity against CYP2C9 (IC50 = 2.77 μM) and CYP2C19 (IC50 = 2.03 μM) in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NLRP3/URAT1-IN-1 (2 mg/kg, p.o., daily, 3 days) significantly reduces ankle swelling in rats with acute gouty arthritis induced by intra-articular injection of MSU crystals[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:3-week-old healthy Kunming (KM) mice with acute hyperuricemia (HUA) induced by hypoxanthine and potassium oxonate[1]
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Dosage:2 mg/kg
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Administration:p.o., single dose
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Result:Reduced serum uric acid (SUA) levels.
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Animal Model:7-8-week-old male Sprague-Dawley (SD) rats (180-220 g) with acute gouty arthritis induced by intra-articular injection of MSU crystals[1]
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Dosage:2 mg/kg
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Administration:p.o., daily, 3 days
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Result:Reduced ankle swelling and IL-1β release.
Chemical Information
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CAS No. 2994637-53-3
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Molecular Weight 525.44
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Formula C24H17BrN2O3S2
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SMILES
O=C(C(N1CC2=C3C=CC=CC3=C(Br)C=C2)=CC4=C1C=CC=C4)NS(=O)(C5=CC=CS5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NLRP3/URAT1-IN-1 Related Classifications
HY-175645 Related Classifications
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