TRP Channel

Inhibitory Selectivity

Isoform-specific Inhibitors

TRP Channel Products

New TRP Channel Products
Catalog No. Information Product Use Citations Product Validations
S8691

ML204

ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels.

S9926New

ML-SA1

ML-SA1 (Mucolipin synthetic agonist 1) is an activator of TRPML channels. ML-SA1 also inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 values of ML-SA1 against DENV2 RNA and ZIKV RNA are 8.93 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral.

E0028New

9-Phenanthrol

9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5.

S6070New

CBA (TRPM4-IN-5)

CBA (TRPM4-IN-5, Compound 5) is a highly selective blocker of the TRPM4 ion channel with an IC50 of 1.5μM.

S0750

GFB-8438

GFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as well as limited activity against the hERG channel.

S0977

AC1903

AC1903 (compound 2) is a specific and selective TRPC5 (transient receptor potential canonical channel 5) inhibitor with IC50 of 4.06 μM.

S6634

SAR7334

SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment.

S8367

GSK2193874

GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively.

S6947New

MK6-83

MK6-83 is a novel Transient receptor potential melastatin member 1 (TRPML1) activator that may be used as a potential pharmacological treatment option for a specific subgroup of MLIV patients.

S8639

Diphenyleneiodonium chloride (DPI)

Diphenyleneiodonium chloride (DPI) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor. Diphenyleneiodonium chloride (DPI) also functions as a TRPA1 activator and selectively inhibits intracellular reactive oxygen species (ROS).

S7848New

QX-314 chloride

QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.

S8073

Optovin

Optovin is a reversible photoactivated TRPA1 activator.

S6657

2-Aminoethyl Diphenylborinate (2-APB)

2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.

S8107

GSK1016790A

GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.

S3942

Cardamonin

Cardamonin (Alpinetin chalcone), isolated from the fruits of Alpinia species, is a chalconoid with anti-inflammatory and anti-tumor activity. It has been shown to be a novel antagonist of hTRPA1 cation channel with IC50 of 454 nM while does not interact with TRPV1 nor TRPV4 channel.

S6638

AMG-333

AMG-333 is a potent and highly selective antagonist of TRPM8 with IC50 values of 13 nM and 30 nM for human TRPM8 and rat TRPM8.

S6934New

AMG-9810

AMG-9810 is potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.

S6637

HC-067047

HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively.

S8137

Capsazepine

Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.

S6838

BCTC

BCTC is an orally effective and highly potent vanilloid receptor 1 (VR1/TRPV1) antagonist. BCTC inhibits capsaicin-induced and acid-induced activation of rat VR1 with IC50 of 35 nM and 6.0 nM, respectivley. BCTC exhibits anti-tumor activity.

S0174

TRPM8 antagonist 2

TRPM8 antagonist 2 (TRPM8 Antagonist) is a potent and selective antagonist of TRPM8 with IC50 of 0.2 nM that can be used for the pharmacological treatment of neuropathic pain syndromes.

S8238

SB366791

SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM.

S3867

(E)-Cardamonin

(E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-kB inhibitor.

S2650

RN-1734

RN-1734 (TRPV4 Antagonist I) is a selective transient receptor potential vanilloid 4 (TRPV4) antagonist with IC50 of 2.3 μM, 5.9 μM and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1734 alleviates demyelination and inhibits glial activation and the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.

S0825

MDR-652

MDR-652 is a potent and specific agonist of transient receptor potential vanilloid 1 (TRPV1) with Ki of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively. MDR-652 has excellent and dose-dependent analgesic activity.

Catalog No. Information Product Use Citations Product Validations
S8691

ML204

ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels.

S9926New

ML-SA1

ML-SA1 (Mucolipin synthetic agonist 1) is an activator of TRPML channels. ML-SA1 also inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 values of ML-SA1 against DENV2 RNA and ZIKV RNA are 8.93 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral.

E0028New

9-Phenanthrol

9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5.

S6070New

CBA (TRPM4-IN-5)

CBA (TRPM4-IN-5, Compound 5) is a highly selective blocker of the TRPM4 ion channel with an IC50 of 1.5μM.

S0750

GFB-8438

GFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as well as limited activity against the hERG channel.

S0977

AC1903

AC1903 (compound 2) is a specific and selective TRPC5 (transient receptor potential canonical channel 5) inhibitor with IC50 of 4.06 μM.

S6634

SAR7334

SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels.SAR7334 blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment.

S8367

GSK2193874

GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively.

Catalog No. Information Product Use Citations Product Validations
S6947New

MK6-83

MK6-83 is a novel Transient receptor potential melastatin member 1 (TRPML1) activator that may be used as a potential pharmacological treatment option for a specific subgroup of MLIV patients.

S8639

Diphenyleneiodonium chloride (DPI)

Diphenyleneiodonium chloride (DPI) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor. Diphenyleneiodonium chloride (DPI) also functions as a TRPA1 activator and selectively inhibits intracellular reactive oxygen species (ROS).

S7848New

QX-314 chloride

QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.

S8073

Optovin

Optovin is a reversible photoactivated TRPA1 activator.

S6657

2-Aminoethyl Diphenylborinate (2-APB)

2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.

S8107

GSK1016790A

GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.

Catalog No. Information Product Use Citations Product Validations
S3942

Cardamonin

Cardamonin (Alpinetin chalcone), isolated from the fruits of Alpinia species, is a chalconoid with anti-inflammatory and anti-tumor activity. It has been shown to be a novel antagonist of hTRPA1 cation channel with IC50 of 454 nM while does not interact with TRPV1 nor TRPV4 channel.

S6638

AMG-333

AMG-333 is a potent and highly selective antagonist of TRPM8 with IC50 values of 13 nM and 30 nM for human TRPM8 and rat TRPM8.

S6934New

AMG-9810

AMG-9810 is potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.

S6637

HC-067047

HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively.

S8137

Capsazepine

Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.

S6838

BCTC

BCTC is an orally effective and highly potent vanilloid receptor 1 (VR1/TRPV1) antagonist. BCTC inhibits capsaicin-induced and acid-induced activation of rat VR1 with IC50 of 35 nM and 6.0 nM, respectivley. BCTC exhibits anti-tumor activity.

S0174

TRPM8 antagonist 2

TRPM8 antagonist 2 (TRPM8 Antagonist) is a potent and selective antagonist of TRPM8 with IC50 of 0.2 nM that can be used for the pharmacological treatment of neuropathic pain syndromes.

S8238

SB366791

SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM.

S3867

(E)-Cardamonin

(E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-kB inhibitor.

S2650

RN-1734

RN-1734 (TRPV4 Antagonist I) is a selective transient receptor potential vanilloid 4 (TRPV4) antagonist with IC50 of 2.3 μM, 5.9 μM and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1734 alleviates demyelination and inhibits glial activation and the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.

Catalog No. Information Product Use Citations Product Validations
S0825

MDR-652

MDR-652 is a potent and specific agonist of transient receptor potential vanilloid 1 (TRPV1) with Ki of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively. MDR-652 has excellent and dose-dependent analgesic activity.