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TRPV4 antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Reference Standards (2) TRP Channel (19)
By Research Areas:	Cancer (4) Cardiovascular Disease (6) Inflammation/Immunology (3) Metabolic Disease (3) 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-100720

GSK2193874 15+ Cited Publications	TRP Channel	Cardiovascular Disease
GSK2193874 is an orally active, potent, and selective *TRPV4* antagonist with IC₅₀s of 2 nM and 40 nM for rTRPV4 and hTRPV4 .

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-19975

RN-1734 5+ Cited Publications	TRP Channel	Neurological Disease Cancer
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC₅₀s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM) . RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells .

HY-18662

RQ-00203078 5+ Cited Publications	TRP Channel	Neurological Disease Cancer
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC₅₀s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels .

HY-19976

RN-1747 5 Publications Verification	TRP Channel	Cardiovascular Disease Metabolic Disease
RN-1747 is a selective *TRPV4* channel agonist, with EC₅₀ values of 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1747 acts as an antagonist of TRPM8, with an IC₅₀ of 4 μM. Topical cutaneous administration of RN-1747 induces hypothermia, increases tail heat loss via cutaneous vasodilation, and promotes cold-seeking behavior in rats. Intracerebroventricular administration of RN-1747 does not induce hypothermia in rats .

HY-160603

PF-05214030	TRP Channel	Others
PF-05214030 is a *TRPV4* antagonist (IC₅₀: 4 and 27nM for hTRPV4 and rTRPV4 respectively). PF-05214030 reverses the reduction in bladder capacity caused by intravesical infusion of a TRPV4 agonist .

HY-160900

RN-1665 1 Publications Verification	TRP Channel	Others
RN-1665 is an orally active *TRPV4* antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively .

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-142620

TRPV4 antagonist 3	TRP Channel	Cardiovascular Disease
TRPV4 antagonist 3 is a *TRPV4* antagonist (pIC₅₀ = 8.4).

HY-185006

TRPV4 antagonist 5	TRP Channel	Others
TRPV4 antagonist 5 (Example 21) is a *TRPV4* antagonist .

HY-112202

GSK3395879	TRP Channel	Cardiovascular Disease
GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC₅₀ of 1 nM for hTRPV4 .

HY-110270

RN-9893	TRP Channel	Inflammation/Immunology
RN-9893 is a potent and selective TRPV4 receptor antagonist with IC₅₀ values of 320, 420 and 660 nM for mouse, human and rat channels, respectively .

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-117372

DFL23448	TRP Channel	Metabolic Disease
DFL23448 is a selective transient receptor potential melastatin-8 (TRPM8) antagonist. DFL23448 shows IC₅₀ values of 10 and 21 nM in hTRPM8 human embryonic kidney 293 cells activated by Cooling Agent 10 or cold. DFL23448 has limited activity (IC₅₀ >10 μM) at transient receptor potential vanilloids TRPV1, TRPA1, or TRPV4 or at various G protein-coupled receptors. DFL23448 can modify bladder function and reduce bladder overactivity in awake rats .

HY-110270A

RN-9893 hydrochloride	TRP Channel	Inflammation/Immunology
RN-9893 Hydrochloride is an orally active antagonist of transient receptor potential vanilloid 4 (TRPV4), with IC₅₀ values of 0.42 and 0.66 μM, for humans and rats, respectively .

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-183906

GSK3491943	TRP Channel	Cardiovascular Disease
GSK3491943 is an antagonist of the transient receptor potential vanilloid subtype 4 (TRPV4) ion channel. GSK3491943 is applicable to research related to pulmonary edema induced by heart failure .

HY-100720R

GSK2193874 (Standard)	TRP Channel Reference Standards	Cardiovascular Disease
GSK2193874 (Standard) is the analytical standard of GSK2193874 (HY-100720). This product is intended for research and analytical applications. GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50s of 2 nM and 40 nM for rTRPV4 and hTRPV4 .

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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 antagonist

Inhibitors & Agonists