2. Membrane Transporter/Ion Channel
  3. GLUT URAT1
  4. URAT1/GLUT9-IN-1

URAT1/GLUT9-IN-1(compound 29) can inhibit both uric acid transporter 1(URAT1)(IC50=2.01 μM) and glucose transporter 9(GLUT9)(IC50=18.21 μM). URAT1/GLUT9-IN-1 exhibits favorable pharmacokinetic properties and oral bioavailability. URAT1/GLUT9-IN-1 can be uesd for gout and hyperuricemia research.

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URAT1/GLUT9-IN-1 Chemical Structure

URAT1/GLUT9-IN-1 Chemical Structure

CAS No. : 2883011-18-3

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URAT1/GLUT9-IN-1 Related Antibodies

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Description

URAT1/GLUT9-IN-1(compound 29) can inhibit both uric acid transporter 1(URAT1)(IC50=2.01 μM) and glucose transporter 9(GLUT9)(IC50=18.21 μM). URAT1/GLUT9-IN-1 exhibits favorable pharmacokinetic properties and oral bioavailability. URAT1/GLUT9-IN-1 can be uesd for gout and hyperuricemia research[1].

IC50 & Target[1]

GLUT9

18.21 μM (IC50)

In Vitro

URAT1/GLUT9-IN-1 possesses the most effective inhibition of URAT1-mediated 14C-uric acid uptake (IC50= 2.01 μM), which is about three times more potent than Lesinurad(HY-15258) (IC50= 5.54 μM)[1].
URAT1/GLUT9-IN-1 (5 μM) compares to Benzbromarone(HY-B1135) at a concentration of 5 μM and demonstrated an IC50 value of 18.21 ± 1.03 μM[1].
URAT1/GLUT9-IN-1 (10 μM) inhibits to xanthine oxidase(XOD) less than 20%, indicating its negligible inhibitory activity[1].
URAT1/GLUT9-IN-1 inhibits the inhibitory potential of CYP drug metabolizing enzymes(CYP2C9 (IC50= 2.00 μM) and CYP2C19 (IC50= 5.93 μM)) and exhibits a low potential for inducing hepatotoxicity[1].

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

URAT1/GLUT9-IN-1 Related Antibodies
In Vivo

URAT1/GLUT9-IN-1 (0.25, 0.5, 1mg/kg, po.) has the smallest effective dose of reduce serum uric acid(SUA) activity is about 0.5 mg/kg in the mouse model of acute hyperuricemia[1].
URAT1/GLUT9-IN-1 (2mg/kg, po.) exhibits significant potential as a SUA reduction drug, demonstrating approximately 1.8-fold higher potency compared to Lesinurad(HY-15258) in a stable hyperuricemia rat model[1].
URAT1/GLUT9-IN-1 (100 mg/kg, po.; every other day for a period of 14 days) displays significantly enhanced safety profiles compared to Lesinurad(HY-15258) in Mice with Chronic Hyperuricemia[1].
Pharmacokinetic Analysis in AD rats[1]

Route Dose (mg/kg) AUC0_t (ng•h/mL) AUC0_INF (ng•h/mL) MRT0_INF (h) T1/2 (h) Tmax (h) Cmax (ng/mL) Cl (L•h/kg) F (%)
p.o. 2 1813.4 7929.1 2.5 1.8 0.25 1272.7 / 20.1
i.v. 2 1903.7 1922.9 0.5 1.6 0.083 6591.8 17.5 /

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

Animal Model: stable hyperuricemia rat model
Dosage: 2 mg/kg
Administration: Oral gavage (p.o.)
Result: Had 90.12% titer ratio of decreasing sua activity.
Animal Model: 14-day model of chronic hyperuricemia
Dosage:
Administration: i.g.
Result: Exhibited superior therapeutic efficacy (76.33%) in chronic hyperuricemia in mice compared to lesinurad (33.56%)
Animal Model: Healthy Mice
Dosage: 100 mg/kg every other day for a period of 14 days
Administration: Oral gavage (p.o.)
Result: Caused slight weight loss and mild kidney damage.
Molecular Weight

435.56

Formula

C23H21N3O2S2
CAS No.
Unlabeled CAS

SMILES

O=C(O)CCCSC1=NC(NC2=C3C=CC=CC3=C(C4CC4)C=C2)=C5C(C=CS5)=N1
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-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:

URAT1/GLUT9-IN-12883011-18-3GLUTURAT1Glucose transporter Urate transporter 1SLC22A12Gout and hyperuricemiaURAT1/GLUT9 inhibotorhyperuricemia rat modelInhibitorinhibitorinhibit

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