TRPV1 antagonist 10

Cat. No.: HY-172774 Purity: 98.54%: Data Sheet
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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.

For research use only. We do not sell to patients.

TRPV1 antagonist 10 Chemical Structure

CAS No. : 896584-55-7

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•Related Small Molecules:

•Related Proteins:

View All TRP Channel Isoform Specific Products:

View All Isoforms

TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

View All GLUT Isoform Specific Products:

View All Isoforms

GLUT1 GLUT2 GLUT3 GLUT4

View All Cytochrome P450 Isoform Specific Products:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

View All Interleukin Related Isoform Specific Products:

View All Isoforms

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 IL-18

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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	Route	T_1/2	Plasma Concentration	AUC	MRT	Bioavailability	T_max	Clearance (CL)
Rat	1 mg/kg	i.v.	14.38 h	106.16 ng/mL	121.54 ng·h/mL	13.39 h	100 %	/	/
Rat	3 mg/kg	p.o.	8.27 h	37.94 ng/mL	141.01 ng·h/mL	8.78 h	34.4 %	0.5 h	0.018993 mg·h/L

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.

896584-55-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(OCCO2)=C2C=C1)NC3=CC=C(OCO4)C4=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 70 mg/mL (222.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1818 mL	15.9089 mL	31.8177 mL
5 mM	0.6364 mL	3.1818 mL	6.3635 mL
10 mM	0.3182 mL	1.5909 mL	3.1818 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.54%

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Data Sheet (277 KB) SDS (252 KB)

COA (247 KB) HNMR (170 KB) LCMS (343 KB)

Handling Instructions (2659 KB)

References

[1]. Chunxia Liu, et al., Structure Optimization of Natural Product Piperine to Obtain Novel and Potent Analogs with Anti-inflammation Pain and Urate-Lowering Effect, European Journal of Medicinal Chemistry, 2025, 117649, ISSN 0223-5234

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1818 mL	15.9089 mL	31.8177 mL	79.5444 mL
	5 mM	0.6364 mL	3.1818 mL	6.3635 mL	15.9089 mL
	10 mM	0.3182 mL	1.5909 mL	3.1818 mL	7.9544 mL
	15 mM	0.2121 mL	1.0606 mL	2.1212 mL	5.3030 mL
	20 mM	0.1591 mL	0.7954 mL	1.5909 mL	3.9772 mL
	25 mM	0.1273 mL	0.6364 mL	1.2727 mL	3.1818 mL
	30 mM	0.1061 mL	0.5303 mL	1.0606 mL	2.6515 mL
	40 mM	0.0795 mL	0.3977 mL	0.7954 mL	1.9886 mL
	50 mM	0.0636 mL	0.3182 mL	0.6364 mL	1.5909 mL
	60 mM	0.0530 mL	0.2651 mL	0.5303 mL	1.3257 mL
	80 mM	0.0398 mL	0.1989 mL	0.3977 mL	0.9943 mL
	100 mM	0.0318 mL	0.1591 mL	0.3182 mL	0.7954 mL