2. Membrane Transporter/Ion Channel
  3. URAT1 GLUT
  4. URAT1/GLUT9-IN-2

URAT1/GLUT9-IN-2 (Compound 42) is a selective, orally active URAT1/GLUT9 inhibitor, with an IC50 of 2.81 μM against URAT1 and an IC50 of 12.53 μM against GLUT9. URAT1/GLUT9-IN-2 reduces serum uric acid levels and protects renal function. URAT1/GLUT9-IN-2 can be used in research related to hyperuricemia and hyperuricemic nephropathy.

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URAT1/GLUT9-IN-2

URAT1/GLUT9-IN-2 Chemical Structure

CAS No. : 3051509-32-8

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URAT1/GLUT9-IN-2 Related Antibodies

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Description

URAT1/GLUT9-IN-2 (Compound 42) is a selective, orally active URAT1/GLUT9 inhibitor, with an IC50 of 2.81 μM against URAT1 and an IC50 of 12.53 μM against GLUT9. URAT1/GLUT9-IN-2 reduces serum uric acid levels and protects renal function. URAT1/GLUT9-IN-2 can be used in research related to hyperuricemia and hyperuricemic nephropathy[1].

IC50 & Target[1]

GLUT9

12.53 μM (IC50)

URAT1

2.81 μM (IC50)

In Vitro

URAT1/GLUT9-IN-2 (30 min) potently inhibits URAT1 in HEK293T cells expressing hURAT1, with an IC50 of 2.81 μM[1].
URAT1/GLUT9-IN-2 inhibits GLUT9 in HEK293T cells expressing hGLUT9, with an IC50 value of 12.53 μM[1].
URAT1/GLUT9-IN-2 (10 μM; 15 min) shows no significant xanthine oxidase (XOD) inhibitory activity, with an inhibition rate of only 14.43% at a concentration of 10 μM[1].
URAT1/GLUT9-IN-2 (30 min) inhibits OAT1-mediated transport in HEK293T cells expressing hOAT1, with an IC50 of 7.83 μM. Compared with ZS-24, it exhibits weaker off-target activity and improved selectivity[1].
URAT1/GLUT9-IN-2 (0-50 μM; 3-20 min) does not inhibit CYP1A2, CYP2C19 or CYP2D6, but moderately inhibits CYP2C9 and CYP3A4M, with IC50 values of 1.12 μM and 1.38 μM, respectively[1].

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

URAT1/GLUT9-IN-2 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax Cmax CL Bioavailability
Rat[1] 20 mg/kg p.o. 234778 ng·h/mL 245355 ng·h/mL 4.38 h 5.43 h 6.34 h 0.500 h 54200 ng/mL / 51.3 %
Rat[1] 2 mg/kg i.v. 44737 ng·h/mL 47833 ng·h/mL 2.27 h 4.91 h 5.55 h 0.0833 h 36400 ng/mL 43.7 mL/h/kg /
In Vivo

URAT1/GLUT9-IN-2 (0.5-1 mg/kg; p.o.; single administration) exhibits potent urate-lowering efficacy in KM mice with acute hyperuricemia[1].
URAT1/GLUT9-IN-2 (2 mg/kg; p.o.; single administration) exhibits potent hypouricemic activity in acute hyperuricemic SD rats, reducing serum uric acid (SUA) by 89.25% at an oral dose of 2 mg/kg[1].
URAT1/GLUT9-IN-2 (2 mg/kg; i.p.; once daily; for 7 consecutive days) reduces serum uric acid levels and protects renal function in hyperuricemic nephropathy KM mice[1].

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

Animal Model: Kunming (KM) mice (male)[1]
Dosage: 1 mg/kg; 0.5 mg/kg
Administration: p.o.; single dose
Result: Reduced SUA with a DR of 80.25% at 1 mg/kg.
Reduced SUA with a DR of 11.98% at 0.5 mg/kg.
Animal Model: Sprague-Dawley (SD) rats[1]
Dosage: 2 mg/kg
Administration: p.o.; single dose
Result: Reduced SUA with a DR of 89.25%.
Animal Model: Kunming (KM) mice (male)[1]
Dosage: 2 mg/kg
Administration: i.p.; daily; 7 days
Result: Significantly reduced SUA levels.
Decreased BUN and CRE levels.
Reduced kidney mass and kidney/body weight ratio.
Prevented renal edema/whitening compared to the model group.
Molecular Weight

475.52

Formula

C25H21N3O5S
CAS No.
SMILES

O=C(NS(=O)(C1=CC=CC([N+]([O-])=O)=C1)=O)C2=CC=CN2CC3=C4C=CC=CC4=C(C=C3)C5CC5
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
References
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URAT1/GLUT9-IN-2 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/GLUT9-IN-23051509-32-8URAT1GLUTUrate transporter 1SLC22A12Glucose transporterhyperuricemiaCYP2D6hyperuricemic nephropathyOAT1GLUT9CYP2C9HEK293T cellsCYP1A2CYP2C19Inhibitorinhibitorinhibit

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