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TRPC antagonist

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By Targets:	Akt (2) Apoptosis (2) Autophagy (2) Calcium Channel (2) CaMK (2) CRAC Channel (2) HCV (2) HCV Protease (2) Histamine Receptor (2) Isotope-Labeled Compounds (1) Na+/Ca2+ Exchanger (2) Sigma Receptor (3) TRP Channel (13)
By Research Areas:	Cancer (5) Cardiovascular Disease (2) Endocrinology (2) Inflammation/Immunology (5) Neurological Disease (7)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100001

SKF-96365 (hydrochloride) Maximum Cited Publications 27 Publications Verification	TRP Channel CRAC Channel Autophagy CaMK Akt Apoptosis Na+/Ca2+ Exchanger Calcium Channel	Neurological Disease Inflammation/Immunology Cancer
SKF-96365 hydrochloride is a *TRPC* channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of *TRPC6, STIM1* and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .

HY-111925

BI-749327 15+ Cited Publications	TRP Channel	Cardiovascular Disease
BI-749327 is a potent, high selectivity and orally bioavailable *TRPC6* antagonist, with IC₅₀s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .

HY-112302

HC-070 5+ Cited Publications	TRP Channel	Neurological Disease
HC-070 is an antagonist of *TRPC4/TRPC5, with IC₅₀*s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.

HY-30234A

Clemizole hydrochloride 1 Publications Verification	Histamine Receptor TRP Channel HCV Protease HCV	Inflammation/Immunology Endocrinology Cancer
Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole hydrochloride is an inhibitor of TRPC5 channel. The IC₅₀ of Clemizole hydrochloride for RNA binding by NS4B is 24 nM, whereas its EC₅₀ for viral replication is 8 μM.

HY-18101A

BD-1063 dihydrochloride 3 Publications Verification	Sigma Receptor TRP Channel	Neurological Disease
BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against *TRPC5* and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .

HY-132813

Evifacotrep	TRP Channel	Neurological Disease
Evifacotrep, a short transient receptor potential channel 5 and 4 (TRPC5/TRPC4) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases. Evifacotrep targets to *TRPC5/TRPC4* with IC₅₀s ≤50 nM .

HY-30234

Clemizole 1 Publications Verification	Histamine Receptor TRP Channel HCV Protease HCV	Inflammation/Immunology Endocrinology Cancer
Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole is an inhibitor of TRPC5 channel. The IC₅₀ of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC₅₀ for viral replication is 8 µM.

HY-125942

SKF-96365 Maximum Cited Publications 27 Publications Verification	CRAC Channel TRP Channel CaMK Akt Apoptosis Autophagy Na+/Ca2+ Exchanger Calcium Channel	Neurological Disease Inflammation/Immunology Cancer
SKF-96365 is a *TRPC* channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of *TRPC6, STIM1* and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .

HY-162090

TRPC antagonist 1	TRP Channel	Cancer
TRPC antagonist 1 (compound 15g) is a potent TRP channel (TRPC) antagonist with IC₅₀s of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM for TRPC3, TRPC4, TRPC5, TPRC6, and TRPC7, respectively. TRPC antagonist 1 displays noteworthy anti-glioblastoma efficacy in vitro against U87 cell lines .

HY-121519

GSK2332255B	TRP Channel	Cardiovascular Disease
GSK2332255B is a potent, selective *TRPC3* and *TRPC6* antagonist with IC₅₀s of 5 nM and 4 nM for rat *TRPC3* and rat *TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC*3/6 over other calcium-permeable channels .

HY-172600

TRPC6 antagonist-1	TRP Channel	Inflammation/Immunology
TRPC6 antagonist-1 (X26) is a *TRPC6* antagonist with IC₅₀ values of 0.97 μM, 3.93 μM, 5.77 μM and 4.37 μM for *TRPC6, TRPC3, TRPC5* and *TRPC7, respectively. TRPC6 antagonist*-1 inhibits TGF-β1-induced myofibroblast differentiation, and attenuates renal fibrosis .

HY-18101

BD-1063	Sigma Receptor TRP Channel	Neurological Disease
BD-1063 is a selective σ-1 receptor antagonist with inhibitory activity against *TRPC5* and TRPM3. BD-1063 exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .

HY-18101S

BD-1063-d8 dihydrochloride	Isotope-Labeled Compounds Sigma Receptor TRP Channel	Neurological Disease
BD-1063-d₈ dihydrochloride is the deuterium labeled BD1063 dihydrochloride (HY-18101A) . BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against *TRPC5* and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .

Cat. No.	Product Name	Chemical Structure

HY-18101S

BD-1063-d8 dihydrochloride
BD-1063-d₈ dihydrochloride is the deuterium labeled BD1063 dihydrochloride (HY-18101A) . BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against *TRPC5* and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .

BD-1063-d8 dihydrochloride

BD-1063-d₈ dihydrochloride is the deuterium labeled BD1063 dihydrochloride (HY-18101A) . BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .

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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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