2. Immunology/Inflammation Membrane Transporter/Ion Channel
  3. NOD-like Receptor (NLR) URAT1 Interleukin Related OAT GLUT
  4. 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.

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NLRP3/URAT1-IN-1

NLRP3/URAT1-IN-1 Chemical Structure

CAS No. : 2994637-53-3

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NLRP3/URAT1-IN-1 Related Antibodies

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NLRP3 NLRP1 NOD1 NOD2

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Description

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[1].

IC50 & Target[1]

IL-1β

2.61 μM (IC50)

NLRP3

 

OAT4

6.08 μM (IC50)

URAT1

3.81 μM (IC50)

GLUT9

11.02 μM (IC50)

In Vitro

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 Related Antibodies
In Vivo

NLRP3/URAT1-IN-1 (Compound 32) (2 mg/kg, p.o., single dose) significantly reduces serum uric acid (SUA) levels in mice with acute hyperuricemia (HUA) induced by Hypoxanthine (HY-N0091) and Potassium oxonate (HY-17511)[1].
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.

Animal Model: 3-week-old healthy Kunming (KM) mice with acute hyperuricemia (HUA) induced by hypoxanthine and potassium oxonate[1]
Dosage: 2 mg/kg
Administration: p.o., single dose
Result: Reduced serum uric acid (SUA) levels.
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]
Dosage: 2 mg/kg
Administration: p.o., daily, 3 days
Result: Reduced ankle swelling and IL-1β release.
Molecular Weight

525.44

Formula

C24H17BrN2O3S2
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NLRP3/URAT1-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NLRP3/URAT1-IN-12994637-53-3NOD-like Receptor (NLR)URAT1Interleukin RelatedOATGLUTUrate transporter 1SLC22A12ILOrganic anion transporterGlucose transporterInhibitorinhibitorinhibit

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