| FB16659 |
WS 3
|
39711-79-0 |
WS 3 is an agonist of TRPM8 with an EC50 of 3.7 μM. |
| FB07495 |
Vanillyl Alcohol
|
498-00-0 |
Vanillyl alcohol is a free radical scavenger with anticonvulsive and bile secretion promoting effect. It can be extracted from the herbs of Gastrodia elata Bl.. |
| FB17562 |
TRPM8 antagonist 14
|
259674-19-6 |
TRPM8 antagonist 14 is a tryptophan-derived selective TRPM8 antagonist with IC50 value of 0.2nM. It showed significant target coverage in both an icilin-induced WDS (at 1-30 mg/kg s.c.) and oxaliplatin-induced cold allodynia (at 0.1-1 μg s.c.) mice models. |
| FB08634 |
SN 2
|
823218-99-1 |
SN 2 is a potent activator of TRPML3 ion channel with EC50 of 1.8±0.13 μM. |
| FB16664 |
9-Phenanthrol
|
484-17-3 |
Selective TRPM4 blocker (IC50 = 20 μM in HEK293 cells). Exhibits no effect on CFTR or TRPM5 (at 0.25 and 1 mM respectively). Abolishes arrhythmias induced by hypoxia in a mouse heart model. |
| FB06714 |
SB-705498
|
501951-42-4 |
SB-705498 is a selective antagonist of transient receptor potential vanilloid 1 (TRPV1) with pIC50 of 7.1. |
| FB05530 |
SB-366791
|
472981-92-3 |
SB-366791 is an antagonist of vanilloid receptor VR1 or TRPV1 with IC50 of 5.7±1.2 nM. |
| FB09872 |
SAR7334
|
1333210-07-3 |
SAR7334 is a potent TRPC6 (Transient receptor potential cation channel, subfamily C, member 6) inhibitor. |
| FB02677 |
RQ-00203078
|
1254205-52-1 |
RQ-00203078 is a selective antagonist of TRPM8 with IC50 of 8.3 nM. |
| FB07152 |
RN-1734
|
946387-07-1 |
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50 values for all three species (hTRPV4: IC50 = 2.3 μM, mTRPV4: IC50 = 5.9 μM, rTRPV4: IC50 = 3.2 μM). |
| FB04834 |
Pyr6
|
245747-08-4 |
Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 μM (Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells). |
| FB02737 |
Pyr10
|
1315323-00-2 |
Pyr 10 is a TRPC3-selective inhibitor. IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM. |
| FB20296 |
A 425619
|
581809-67-8 |
Potent TRPV1 antagonist. |
| FB11356 |
AM-0902
|
1883711-97-4 |
Potent and selective TRPA1 antagonist (IC50 = 0.02 μM for human TRPA1). Exhibits no siginificant activity against human TRPV1 or TRPV4, and rat TRPV1, TRPV3 or TRPM8. Exhibits efficacy in a rat pain model. Orally bioavailable. |
| FB10336 |
Podocarpic Acid
|
5947-49-9 |
Podocarpic acid is a natural product, which has the best all-round positive effect and acts as a TRPA1 activator. |
| FB11286 |
PF-05105679
|
1398583-31-7 |
PF-05105679 is an orally-bioavailable and selective TRPM8 blocker (IC50 = 103 nM) which exhibits > 100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. |
| FB01658 |
Optovin
|
348575-88-2 |
Optovin is a reversible and photoactive activator of TRPA1 with EC50 of 2 μM in wild-type zebrafish. |
| FB17168 |
OLDA
|
105955-11-1 |
OLDA is an agonist of endogenous vanilloid TRPV1 (VR1) receptor with EC50 of 36 nM and low affinity for rCB1 receptors (Ki = 1.6 μM). |
| FB00684 |
Nonivamide
|
2444-46-4 |
Nonivamide, an analog of capsaicin, is agonist of transient receptor potential vanilloid type 1 (TRPV1). It can be extracted from the fruits of Capsicum annuum L.. |
| FB11103 |
MRS1477
|
212200-21-0 |
MRS1477 is a positive allosteric modulator of TRPV1 channels targeting breast cancer cells. |
| FB08082 |
ML204
|
5465-86-1 |
ML204 is a selective antagonist of TRPC4 ion channel with IC50 of 0.96 μM and 2.6 μM in fluorescent and electrophysiological assays respectively. |
| FB10331 |
ML204 HCl
|
2070015-10-8 |
ML204 HCl is a potent, selective TRPC4 channel inhibitor with IC50 of 0.96 μM. |
| FB17208 |
MDR-652
|
1933528-96-1 |
MDR-652 is a high-affinity TRPV1 agonist with Ki value of 11.4nM. |
| FB07160 |
Mavatrep
|
956274-94-5 |
Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6. |
| FB17265 |
Linoleylethanolamide
|
68171-52-8 |
Linoleylethanolamide is an endocannabinoid agent. It acts by binding to TRPV1, increasing ERK phosphorylation and AP-1 dependent transcription in CB-receptor in an independent manner. |
| FB12035 |
JYL 1421
|
401907-26-4 |
JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM. |
| FB06299 |
JNJ-17203212
|
821768-06-3 |
JNJ-17203212 is a selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1. |
| FB04416 |
Icilin
|
36945-98-9 |
Icilin is an agonist of TRPM8 ion channel with EC50 of 0.36 μM in HEK 293 cells. |
| FB06894 |
HC-067047
|
883031-03-6 |
HC-067047 is a TRPV4 antagonist with IC50 value of 48 ± 6 nM in human. |
| FB06140 |
HC-030031
|
349085-38-7 |
HC-030031 is a blocker of TRPA1 channel that exhibits antagonistic effect on AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively. |
| FB10934 |
GSK2193874
|
1336960-13-4 |
GSK2193874 is a selective transient receptor potential vanilloid 4 (TRPV4) blocker with IC50 value of 0.04 μM. |
| FB06980 |
GSK1016790A
|
942206-85-1 |
GSK1016790A is a potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells. |
| FB16523 |
GFB-8438
|
2304549-73-1 |
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. |
| FB16654 |
EIPA
|
1154-25-2 |
EIPA (L593754) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis. |
| FB16878 |
Eact
|
461000-66-8 |
Eact is an activator of TMEM16A calcium-activated chloride channel (CaCC) with EC50 of 3 μM. It is also transient receptor potential vanilloid 1 (TRPV1) channel activator (EC50 = 11.6 μM). |
| FB10333 |
D-3263 HCl
|
1008763-54-9 |
D-3263 HCl is an orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist. |
| FB04902 |
Chembridge-5861528
|
332117-28-9 |
Chembridge-5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively). |
| FB11287 |
Cannabidivarin
|
24274-48-4 |
Cannabidivarin is a non-psychoactive cannabinoid found in Cannabis that activates CB2 cannabinoid receptors as well as the transient receptor potential channels TRPA1, TRPV1, and TRPV2 (EC50s = 0.42, 3.6, and 7.3 µM, respectively). It is also reported to antagonize TRPM8 (IC50 = 0.9 µM) and to inhibit diacylglycerol lipase (IC50 = 16.6 µM). |
| FB06049 |
Bisandrographolide A
|
160498-00-0 |
Bisandrographolide A, a natural product, activates TRPV4 channels, could play a role in some of the effects of Andrographis extract described in traditional medicine. |
| FB15538 |
β-Eudesmol
|
473-15-4 |
Beta-Eudesmol is a natural oxygenated sesquiterpene, activates hTRPA1, with an EC50 of 32.5 μM. Beta-Eudesmol increases appetite through TRPA1[1]. |
| FB04417 |
BCTC
|
393514-24-4 |
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells. |
| FB11262 |
ASP 7663
|
1190217-35-6 |
ASP 7663 is an orally-bioavailabe, selective TRPA1 activator (EC50 values are ~0.5 μM in human, mouse and rat), which displays little or no affinity at more than 60 other related receptors, channels and enzymes. It stimulates 5-HT release from QGP-1 cells and exhibits an abdominal analgesic effect in vivo. |
| FB16880 |
Arvanil
|
128007-31-8 |
Arvanil is an antagonist of cannabinoid CB1 and vanilloid TRPV1 (VR1) with Ki values are 0.5 and 0.3 μM respectively. |
| FB07889 |
AMG9810
|
545395-94-6 |
AMG9810 is an antagonist of TRPV1 receptor with IC50 of 17 nM and exhibits antihyperalgesic properties in rat model. |
| FB16764 |
AMG-9090
|
118215-82-0 |
AMG-9090 is a transient receptor potential ankyrin 1 (TRPA1) antagonist. |
| FB06711 |
AMG-517
|
659730-32-2 |
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. |
| FB15650 |
AMG 333
|
1416799-28-4 |
AMG 333 is a potent and selective TRPM8 antagonist with IC50 value of 13nM. |
| FB15674 |
AC1903
|
831234-13-0 |
AC1903 is an inhibitor of transient receptor potential canonical channel 5 (TRPC5) with IC50 of 14.7 µM. |
| FB03148 |
A 967079
|
1170613-55-4 |
A 967079 is a selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively). |
| FB12795 |
2-Aminoethyl diphenylborinate
|
524-95-8 |
2-Aminoethyl diphenylborinate is an antagonist of membrane permeable IP3 receptor and a blocker of broad TRP channels including TRPC5 and TRPM2. |