2. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. TRP Channel URAT1 GLUT Cytochrome P450 Interleukin Related TNF Receptor
  4. TRPV1 antagonist 10

TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC50 = 33.06 nM), moderate to weak URAT1 (IC50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.

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TRPV1 antagonist 10 Chemical Structure

TRPV1 antagonist 10 Chemical Structure

CAS No. : 896584-55-7

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TRPV1 antagonist 10 Related Antibodies

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TRPC TRPM TRPV TRPA TRPML

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GLUT1 GLUT2 GLUT3 GLUT4

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC50 = 33.06 nM), moderate to weak URAT1 (IC50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain[1].

IC50 & Target[1]

TRPV1

36.47 nM (IC50)

TRPV3

>100 μM (IC50)

TRPV4

>100 μM (IC50)

TRPA1

>100 μM (IC50)

TRPM8

6.47 μM (IC50)

CYP1A2

28.31 μM (IC50)

CYP2C9

42.85 μM (IC50)

CYP2C19

9.23 μM (IC50)

CYP2D6

>100 μM (IC50)

CYP3A4M

8.73 μM (IC50)

In Vitro

TRPV1 antagonist 10 (Compound 39) (50 μM, 24 h) shows 60.25% inhibition rate against GLUT9 in UA (1 mM)-treated HEK293T cells[1].
TRPV1 antagonist 10 (0-400 μM, 24-72 h) exhibits higher levels of cytotoxicity on HepG2 and HK2 cells with increasing dose and time of incubation[1].
TRPV1 antagonist 10 (0-100 μM, 3-20 min) shows high metabolic stability in human and rat liver microsomes[1].

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

TRPV1 antagonist 10 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 and HK2 cell lines
Concentration: 0-400 μM
Incubation Time: 24 or 72 h incubation
Result: Exhibited little cytotoxicity in HepG2 cells after 24 h incubation.
Caused significant cytotoxicity at the concentration of 50 μM after 72 h incubation in HepG2 cells.
Led to significant inhibition of cell viability in HK2 cell line at 200 μM and 24 h incubation.
Had slightly less toxicity in both cell lines in comparison to Benzbromaron (HY-B1135).
Parmacokinetics
Species Dose SampleTime Route Indicator value
Rat 1 mg/kg 24 h i.v. T1/2 14.38 hr
Rat 3 mg/kg 24 h p.o. T1/2 8.27 hr
Rat 1 mg/kg 24 h i.v. Cmax 106.16 ng/mL
Rat 3 mg/kg 24 h p.o. Tmax 0.5 hr
Rat 1 mg/kg 24 h i.v. AUC0-t 121.54 ng·h/mL
Rat 3 mg/kg 24 h p.o. Cmax 37.94 ng/mL
Rat 1 mg/kg 24 h i.v. AUC0-inf 153.12 ng·h/mL
Rat 3 mg/kg 24 h p.o. AUC0-t 141.01 ng·h/mL
Rat 1 mg/kg 24 h i.v. MRT 13.39 hr
Rat 3 mg/kg 24 h p.o. AUC0-inf 157.95 ng·h/mL
Rat 1 mg/kg 24 h i.v. F 100 %
Rat 3 mg/kg 24 h p.o. MRT 8.78 hr
Rat 3 mg/kg 24 h p.o. CL/F 0.018993 mg·h/L
Rat 3 mg/kg 24 h p.o. F 34.4 %
In Vivo

TRPV1 antagonist 10 (Compound 39) (3-20 mg/kg, p.o., one single dose) shows dose-dependent analgesic effect in both Formalin-induced phase I and phase II pain in male Kunming mice model[1].
TRPV1 antagonist 10 (10-20 mg/kg, p.o., 21 consecutive days) reduces the uric acid level and improves the renal function at 20 mg/kg in hyperuricemia mice model[1].
TRPV1 antagonist 10 (500 mg/kg, p.o., one single dose) leads to no obvious abnormal behaviors and difference in weight and food intake in healthy Kunming mice[1].
TRPV1 antagonist 10 (100 mg/kg, p.o., every other day for 14 consecutive days) leads to no obvious abnormal behaviors and difference in weight and food intake in healthy Kunming mice[1].

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

Animal Model: Male Kunming mice, 5% Formalin (injected subcutaneously into the right rear toe)-induced persistent pain model (8 weeks, 22-25 g)[1]
Dosage: 3 mg/kg, 10 mg/kg, 20 mg/kg
Administration: Oral gavage (p.o.), one single dose
Result: Showed no obvious anti-nociceptive activity at dose of 3 mg/kg and 10 mg/kg.
Exhibited significantly better analgesic effect with 20 mg/kg dosage in phase I (0-5 min) and phase II (6-45 min) pain.
Animal Model: Male Kunming hyperuricemia mice model (8 weeks, 22-25 g)[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Oral gavage (p.o.), 21 consecutive days
Result: Reduced inflammatory cytokines (IL-1β, TNF-α, and IL-6) with both dosages.
Reduced the level of renal interstitial fibrosis after 21 continuous days.
Molecular Weight

314.29

Formula

C16H14N2O5
CAS No.
SMILES

O=C(NC1=CC(OCCO2)=C2C=C1)NC3=CC=C(OCO4)C4=C3
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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TRPV1 antagonist 10 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:

TRPV1 antagonist 10896584-55-7TRP ChannelURAT1GLUTCytochrome P450Interleukin RelatedTNF ReceptorTransient receptor potential channelsUrate transporter 1SLC22A12Glucose transporter CYPsILTumor Necrosis Factor ReceptorTNFRTRPV1analgesicuric-acidGLUT9hyperuricemiainflammatory paininflammationInhibitorinhibitorinhibit

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