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 ǰȳ  Ű   Pharmacology

Transient Receptor Potential (TRP) Channels Small Molecules

Transient Receptor Potential (TRP) Channels õ small molecule Ұմϴ.

TOCRIS
ǰ ϱ
μϱ




Activators
Cat. No. Product Name / Activity
5178 ASP 7663
Selective TRPA1 activator
1531 Icilin
Activates a novel cold receptor. Cooling agent
6269 JT010
Potent and selective TRPA1 channel activator
4901 Optovin
Reversible photoactive TRPA1 activator
3197 Polygodial
TRPA1 channel activator; analgesic and antifungal
1418 Resveratrol
TRPA1 activator: also cyclooxygenase inhibitor
Blockers
Cat. No. Product Name / Activity
4716 A 967079
Selective TRPA1 channel blocker
5914 AM 0902
Potent and selective TRPA1 antagonist
3296 AP 18
Reversible TRPA1 channel blocker
2896 HC 030031
Selective TRPA1 blocker
3938 TCS 5861528
TRPA1 blocker



Modulators
Cat. No. Product Name / Activity
6875 TRPC6-PAM-C20
Selective TRPC6 positive allosteric modulator
Inhibitors
Cat. No. Product Name / Activity
6495 AM 12
TRPC5 inhibitor
6494 Galangin
TRPC5 inhibitor; also induces autophagy
5831 SAR 7334
Potent TRPC6 inhibitor
Activators
Cat. No. Product Name / Activity
6940 BTD
Selective TRPC5 activator
4522 Flufenamic acid
Activates TRPC6; NSAID
6508 GSK 1702934A
Potent and selective TRPC3/6 activator
0768 Riluzole hydrochloride
TRPC5 activator; also inhibits GABA uptake and glutamate release and blocks NaV channels
Blockers
Cat. No. Product Name / Activity
6766 AC 1903
Selective TRPC5 blocker
5371 Clemizole hydrochloride
TRPC5 blocker; also H1 antagonist
4912 GsMTx4
TRPC1 and TRPC6 blocker; inhibits mechanosensitive ion channels
5807 M 084 hydrochloride
TRPC4/5 channel blocker; antidepressant and anxiolytic
4732 ML 204
Selective TRPC4 blocker
3751 Pyr3
Selective TRPC3 blocker
1147 SKF 96365 hydrochloride
TRPC channel blocker; also inhibits store-operated Ca2+ entry
Others
Cat. No. Product Name / Activity
7013 OptoBI-1
Photoswitchable TRPC3/6/7 agonist


Agonists
Cat. No. Product Name / Activity
5521 CIM 0216
Selective TRPM3 agonist
1531 Icilin
Activates a novel cold receptor. Cooling agent
3040 WS 12
TRPM8 agonist; cooling agent
2927 WS 3
TRPM8 agonist; cooling agent
Antagonists
Cat. No. Product Name / Activity
6874 AMG 333
Potent and selective TRPM8 antagonist; active in vivo
5388 RQ 00203078
Potent and selective TRPM8 antagonist; orally active
5410 TC-I 2014
Potent TRPM8 antagonist
Activators
Cat. No. Product Name / Activity
5376 Pregnenolone sulfate sodium salt
TRPM3 activator; also NMDA potentiator and inhibitor of GABAA receptors
Blockers
Cat. No. Product Name / Activity
3989 AMTB hydrochloride
TRPM8 blocker
6724 CBA
Selective TRPM4 blocker
5324 M8 B hydrochloride
Potent and selective TRPM8 channel blocker
5143 Ononetin
TRPM3 blocker
6003 PF 05105679
Selective TRPM8 blocker
4999 9-Phenanthrol
Selective TRPM4 blocker
4632 TC-I 2000
TRPM8 blocker
Others
Cat. No. Product Name / Activity
1268 U 73122
TRPM4 activator and TRPM3 blocker; also phospholipase C inhibitor



Activators
Cat. No. Product Name / Activity
5547 MK6-83
TRPML channel activator
4746 ML SA1
Activator of TRPML channels
4907 SN 2
Selective TRPML3 channel activator
Blockers
Cat. No. Product Name / Activity
4741 Gadolinium chloride
TRPML3 blocker; stretch-activated calcium channel blocker



Blockers
Cat. No. Product Name / Activity
0890 Amiloride hydrochloride
Na+ channel blocker; inhibits TRPP3 channel
3380 Benzamil
NCX inhibitor; inhibits TRPP3 channel activity
3378 EIPA
Inhibits TRPP3-mediated currents; also inhibits the Na+/H+ exchanger (NHE)
3379 Phenamil
Inhibits TRPP3-mediated currents; also inhibits epithelial Na+ channels



Agonists
Cat. No. Product Name / Activity
1116 AM 404
Vanilloid receptor agonist. Also anandamide transport inhibitor
1339 Anandamide
Endogenous CB and TRPV1 receptor agonist
1354 Arvanil
Potent TRPV1 (VR1) and CB1 agonist/anandamide transport inhibitor
0462 (E)-Capsaicin
Prototypic vanilloid receptor agonist
6433 GSK 1016790A
Potent TRPV4 agonist; active in vivo
1568 NADA
Endogenous TRPV1 agonist. Also CB1 agonist
1641 OLDA
Potent, selective endogenous TRPV1 agonist
0934 Olvanil
Potent vanilloid receptor agonist
1466 PPAHV
Non-pungent vanilloid receptor agonist
3745 RN 1747
Selective TRPV4 agonist
Antagonists
Cat. No. Product Name / Activity
5781 A 425619
Potent TRPV1 antagonist
4319 A 784168
Potent and selective TRPV1 antagonist
4330 AMG 21629
Potent and selective TRPV1 antagonist
5995 AMG 517
Potent TRPV1 antagonist
2316 AMG 9810
Potent and selective, competitive antagonist of TRPV1
2836 Arachidonyl serotonin
Dual FAAH inhibitor/TRPV1 antagonist
3875 BCTC
TRPV1 antagonist
0464 Capsazepine
Vanilloid receptor antagonist; also activator of ENaCδ
5106 GSK 2193874
Potent and selective TRPV4 antagonist; orally active
4100 HC 067047
Potent and selective TRPV4 antagonist
1975 6-Iodonordihydrocapsaicin
Potent, competitive vanilloid receptor antagonist
3361 JNJ 17203212
Reversible, competitive and potent TRPV1 antagonist
1577 L-R4W2
TRPV1 antagonist peptide
3746 RN 1734
Selective TRPV4 antagonist
5678 RN 9893 hydrochloride
Potent and selective TRPV4 antagonist
1439 Ruthenium Red
Blocks capsaicin-activated cation channels
1615 SB 366791
Potent, selective, competitive TRPV1 antagonist
3265 SB 452533
Potent TRPV1 receptor antagonist
4729 α-Spinasterol
TRPV1 antagonist; active in vivo
1098 Tranilast
Antiallergic; inhibits TRPV2-mediated responses
Modulators
Cat. No. Product Name / Activity
5246 MRS 1477
TRPV1 positive allosteric modulator
Activators
Cat. No. Product Name / Activity
4876 Eact
TRPV1 channel activator; also TMEM16A activator
Ligand Sets
Cat. No. Product Name / Activity
2181 Vanilloid TRPV1 Receptor Tocriset™
Selection of 5 vanilloid TRPV1 receptor ligands (Cat. Nos. 0462, 0934, 1137, 0464 and 1615)
Others
Cat. No. Product Name / Activity
5464 AC 4
Photoswitchable TRPV1 channel blocker
2203 PALDA
Endogenous lipid; potentiates effects of endovanilloids at TRPV1 receptors
2204 STEARDA
Endogenous lipid, active in vivo. Enhances effects of endovanilloids at TRPV1 receptors
1684 Tocrisolve™ 100
Water-soluble emulsion; negative control for reagents in TocrisolveTM 100



Antagonists
Cat. No. Product Name / Activity
1224 2-APB
TRP channel modulator. Also IP3 receptor antagonist