2. Membrane Transporter/Ion Channel Immunology/Inflammation Apoptosis
  3. URAT1 Interleukin Related NOD-like Receptor (NLR) Caspase
  4. URAT1-IN-16

URAT1-IN-16 is an orally active URAT1 inhibitor with an IC50 value of 0.19 μM. URAT1-IN-16 also functions as an NLRP3 inflammasome pathway inhibitor by effectively suppressing mature IL-1β secretion (IC50 = 2.52 μM). URAT1-IN-16 exhibits remarkable serum uric acid-lowering and anti-inflammatory activities in vivo, and can be used for hyperuricemia and gout research.

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URAT1-IN-16

URAT1-IN-16 Chemical Structure

CAS No. : 2864442-74-8

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URAT1-IN-16 Related Antibodies

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NLRP3 NLRP1 NOD1 NOD2

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Description

URAT1-IN-16 is an orally active URAT1 inhibitor with an IC50 value of 0.19 μM. URAT1-IN-16 also functions as an NLRP3 inflammasome pathway inhibitor by effectively suppressing mature IL-1β secretion (IC50 = 2.52 μM). URAT1-IN-16 exhibits remarkable serum uric acid-lowering and anti-inflammatory activities in vivo, and can be used for hyperuricemia and gout research[1].

IC50 & Target[1]

URAT1

0.19 μM (IC50)

IL-1b

2.52 μM (IC50)

In Vitro

URAT1-IN-16 (Compound 2) (30 min pre-incubation; 5 min uptake assay) potently inhibits human URAT1-mediated 14C-uric acid uptake in hURAT1-transfected HEK293T cells (IC50 = 0.19 μM)[1].
URAT1-IN-16 (up to 10 μM; 15 min) dose-dependently inhibits mature IL-1β secretion and active Caspase-1 generation in LPS-primed and ATP-stimulated mouse bone marrow-derived macrophages (BMDMs) (IC50 = 2.52 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

URAT1-IN-16 Related Antibodies

ELISA Assay[1]

Cell Line: BMDMs from 6-week-old male C57BL/6 WT mice were treated with LPS (1 μg/mL) and ATP (5 mM)
Concentration: Varying gradient concentrations up to 10 μM
Incubation Time: 15 min
Result: Dose-dependently inhibited mature IL-1β secretion with an IC50 value of 3.39 μM.

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 10 and 20 μM
Incubation Time: 30 min
Result: Reduced the generation of active cleaved caspase-1 in a distinct dose-dependent manner without altered levels of pro-Caspase-1, NEK7, or ASC.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-∞ T1/2 Tmax Cmax F CL
Rat[1] 10 mg/kg p.o. 5072.0 ng/mL·h 5226.7 ng/mL·h 5.0 h 6.3 h 1.0 h 1250.0 ng/mL 20.1 % /
Rat[1] 2 mg/kg i.v. 5190.3 ng/mL·h 5209.7 ng/mL·h 1.1 h 3.3 h / / / 6.4 mL/min/kg
In Vivo

URAT1-IN-16 (Compound 2) (0.25-2 mg/kg; p.o; single dose) significantly lowers serum uric acid (SUA) levels in a mouse model of acute hyperuricemia[1].
URAT1-IN-16 (2 mg/kg; p.o.; single dose) significantly decreases serum uric acid (SUA) levels in a rat model of hyperuricemia[1].
URAT1-IN-16 (500-1500 mg/kg; p.o.; single dose) exhibits high acute safety profiles with a maximum tolerated dose (MTD) above 1000 mg/kg in healthy Kunming mice[1].
URAT1-IN-16 (50 mg/kg; p.o.; every other day; for 28 days) shows favorable subacute tolerance with no organic toxicity or weight differences in healthy Kunming mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse model of acute hyperuricemia (induced by hypoxanthine and potassium oxonate)[1]
Dosage: 0.125, 0.25, 0.5, 1, 2 mg/kg
Administration: Oral gavage (p.o.), single dose
Result: Reduced serum uric acid levels from 1162.0 μM to a normal physiological range of 143.20 μM within 4 h at 2 mg/kg, achieving a 96.8% reduction rate.
Exhibited a clear dose-dependent urate-lowering effect, with reduction rates of 93.4% (1 mg/kg), 72.6% (0.5 mg/kg), and 53.1% (0.25 mg/kg), and established a minimum effective dose of 0.25 mg/kg.
Animal Model: Rat model of hyperuricemia [1]
Dosage: 2 mg/kg
Administration: Oral gavage (p.o.), single dose
Result: Induced a marked reduction in serum uric acid levels from 917.80 μM to 173.80 μM within 4 h post dosing, corresponding to a 91.87% decrease.
Demonstrated cross-species urate-lowering activity and showed over 3-fold superior efficacy compared with lesinurad.
Animal Model: healthy Kunming mice (10-12 g, male and female)[1]
Dosage: 500, 1000, 1500 mg/kg
Administration: Oral gavage (p.o.), single dose
Result: Established a maximum tolerated dose (MTD) above 1000 mg/kg with 100% survival within 1 week.
Showed 80% survival at 1500 mg/kg, with two female mouse deaths occurring within 72 h at the highest dose.
Did not induce observable abnormalities in behavior, posture, appearance, or body weight gain at the MTD.
Animal Model: healthy Kunming mice (10-12 g, male and female)[1]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.), every other day for 28 days
Result: Produced no mortality and no observable adverse behavioral effects (lethargy, convulsion, anorexia, or piloerection) during 28 days of treatment.
Maintained normal body weight gain comparable to vehicle control and showed no significant changes in major organ coefficients.
Did not induce histopathological lesions in heart, liver, spleen, lung, or kidney tissues.
Molecular Weight

607.54

Formula

C28H23BrN4O3S2
CAS No.
SMILES

BrC(C=C1)=CC=C1S(NC(C(C)SC2=NC3=NC=CC=C3N2C4=CC=C(C5CC5)C6=C4C=CC=C6)=O)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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URAT1-IN-16 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:

URAT1-IN-162864442-74-8URAT1Interleukin RelatedNOD-like Receptor (NLR)CaspaseUrate transporter 1SLC22A12ILNLRP3 inflammasomeHyperuricemiaGoutIL-1βCaspase-1BMDMsHyperuricemic mouse modelHyperuricemic rat modelUric acid loweringAnti-inflammatory activityInflammasome inhibitionSerum uric acidInhibitorinhibitorinhibit

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