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TRPV4 inhibitor

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By Targets:	CHIKV (1) Environmental Pollutants (1) Parasite (2) Reference Standards (3) TRP Channel (15)
By Research Areas:	Cancer (4) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (4)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100208

HC-067047 Maximum Cited Publications 41 Publications Verification	TRP Channel	Cancer
HC-067047 is a potent and selective *TRPV4* antagonist and reversibly inhibits currents through the human, rat, and mouse *TRPV4* orthologs with IC₅₀ values of 48 nM, 133 nM, and 17 nM, respectively .

HY-120691A

GSK205 10+ Cited Publications	TRP Channel	Metabolic Disease Inflammation/Immunology
GSK205 is a potent, selective *TRPV4* antagonist with an IC₅₀ of 4.19 μM for inhibiting *TRPV4*-mediated Ca ²⁺ influx .

HY-101507

Zerencotrep 10+ Cited Publications Pico145; HC-608	TRP Channel	Cancer
Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC₅₀s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8 .

HY-116291

4α-Phorbol 12,13-didecanoate 4αPDD	TRP Channel CHIKV	Infection Inflammation/Immunology
4α-Phorbol 12,13-didecanoate (4αPDD) is a transient receptor potential vanilloid 4 (TRPV4) agonist. 4α-Phorbol 12,13-didecanoate can promote Ca ²⁺ influx, induce ATP release and function as an osmoreceptor. 4α-Phorbol 12,13-didecanoate can inhibit water intake and increase maximal micturition pressure in rats. 4α-Phorbol 12,13-didecanoate can be used for the researches of inflammation and infection, such as chikungunya virus (CHIKV) .

HY-B1177

Crotamiton	Environmental Pollutants TRP Channel Parasite	Infection
Crotamiton is a *TRPV4* inhibitor. Crotamiton inhibits *TRPV4* currents. Crotamiton inhibits *TRPV4* selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the *H1R/TRPV1,* MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus .

HY-157131

TRPV2-selective blocker 1 2 Publications Verification	TRP Channel	Neurological Disease
TRPV2-selective blocker 1 is a TRPV2-selective blocker that inhibits calcium influx and ionic currents. TRPV2-selective blocker 1 exhibits an IC₅₀of 6.3 μM against rat *TRPV2, and shows no activity against TRPV1, TRPV3* or *TRPV4* channels. TRPV2-selective blocker 1 attenuates macrophage phagocytosis, LPS-induced macrophage migration, and calcium microdomains generated by peripheral *TRPV2. TRPV2-selective blocker 1 is non-cytotoxic and can be used to investigate the function of TRPV2* during immune processes .

HY-176464

GSK2220691	TRP Channel	Inflammation/Immunology
SK2220691 is a potent *TRPV4* inhibitor. SK2220691 inhibits pulmonary edema induced by GSK1016790. SK2220691 inhibits HCl-induced increases in key factors such as VEGF, keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF) .

HY-149823

TRPV4 antagonist 4	TRP Channel	Neurological Disease
TRPV4 antagonist 4 is a potent *TRPV4* antagonist with an IC₅₀ value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury .

HY-162765

TRPV4-IN-5	TRP Channel	Inflammation/Immunology
TRPV4-IN-5 (Compound 1f) is a potent *TRPV4* inhibitor (IC₅₀ = 0.46 μM). TRPV4-IN-5 significantly alleviates the symptoms of acute lung injury induced by lipopolysaccharide (HY-D1056) in mice .

HY-W721480

HC-067047 hydrochloride	TRP Channel	Neurological Disease
HC-067047 hydrochloride is a potent and selective *TRPV4* antagonist and reversibly inhibits currents through the human, rat, and mouse *TRPV4* orthologs with IC₅₀ values of 48 nM, 133 nM, and 17 nM, respectively .

HY-B1177R

Crotamiton (Standard)	Reference Standards Parasite TRP Channel	Infection
Crotamiton (Standard) is the analytical standard of Crotamiton. This product is intended for research and analytical applications. Crotamiton is a *TRPV4* inhibitor. Crotamiton inhibits *TRPV4* currents. Crotamiton inhibits *TRPV4* selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the *H1R/TRPV1,* MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus .

HY-122692

TRPV4/TRPA1-IN-1	TRP Channel	Neurological Disease Inflammation/Immunology
TRPV4/TRPA1-IN-1 is a *TRPV4/TRPA1* inhibitor that suppresses TRPV4/TRPA1-mediated calcium influx. TRPV4/TRPA1-IN-1 alleviates pain behaviors in a mouse trigeminal stimulation pain model and inhibits inflammation and pain-related behaviors in a mouse acute pancreatitis model. TRPV4/TRPA1-IN-1 can be used in research on acute pancreatitis .

HY-182455

GSK3527497	TRP Channel	Cardiovascular Disease
GSK3527497 is an orally active *TRPV4* inhibitor. GSK3527497 is applicable for the research of heart failure .

HY-100208R

HC-067047 (Standard)	TRP Channel Reference Standards	Cancer
HC-067047 (Standard) is the analytical standard of HC-067047 (HY-100208). This product is intended for research and analytical applications. HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively .

HY-101507R

Zerencotrep (Standard) Pico145 (Standard); HC-608 (Standard)	TRP Channel Reference Standards	Cancer
Zerencotrep (Standard) is the analytical standard of Zerencotrep (HY-101507). This product is intended for research and analytical applications. Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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TRPV4 inhibitor

Inhibitors & Agonists