| S7115 |
AMG-517 |
AMG 517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM， respectively. |
Selective |
TRPV1, IC50: 1 nM-2 nM |
| 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. |
Selective |
hTRPV4, IC50: 0.04 μM; rTRPV4, IC50: 0.002 μM |
| 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. |
Selective |
mTRPV4, IC50: 18 nM; hTRPV4, IC50: 2.1 nM |
| S8238 |
SB366791 |
SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM. |
Selective |
TRPV1, IC50: 5.7 nM |
| 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. |
Selective |
rTRPV1 (capsaicin-induced), IC50: 35 nM; rTRPV1 (acid-induced), IC50: 6.0 nM |
| 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. |
Selective |
hTRPV1, Ki: 11.4 nM; rTRPV1, Ki: 23.8 nM |
| 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. |
Selective |
hTRPV4, IC50: 48 nM; rTRPV4, IC50: 133 nM; mTRPV4, IC50: 17 nM |
| S6934 |
AMG-9810 |
AMG-9810 is a 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 tumorigen |
Selective |
hTRPV1, IC50: 24.5 nM; rTRPV1, IC50: 85.6 nM |
| S2773 |
SB705498 |
SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2. |
Selective |
hTRPV1, pIC50: 7.1; hTRPV1, pKi: 7.6 |
| 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. |
Selective |
hTRPV4, IC50: 2.3 μM; mTRPV4, IC50: 5.9 μM; rTRPV4, IC50: 3.2 μM |
| S4022 |
Probenecid |
Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. Probenecid is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker. |
Selective |
|
| S4516 |
(+)-Camphor |
Camphor is a waxy, flammable, white or transparent solid with a strong aroma, often used to relieve pain, reduce itching and treat fungal infections. It can activate TRPV1 and TRPV3. |
Selective |
|
| S8137 |
Capsazepine |
Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01. |
Selective |
|
| S7848 |
QX-314 chloride |
QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels. |
Pan |
|
| S3756 |
Methyl salicylate |
Methyl salicylate (Betula oil, Gaultheria oil, Methyl 2-hydroxybenzoate, Natural wintergreen oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1. |
Pan |
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