• Home
  • About us
  • Log-In
  • Join Us
  • Sitemap
  • Recruit
ǰ/ Q&A
ֹ
Խ
ڷû
ڷ
Ŭ
A/S
Ŭ ȸ
 ǰȳ  Ű   Pharmacology

Ion Channel Small Molecules

Ion Channel signaling õ small molecule ȳմϴ.

TOCRIS
ǰ ϱ
μϱ




Blockers
Cat. No. Product Name / Activity
5412 TC AQP1 1
Aquaporin 1 (AQP1) channel blocker
5425 TGN 020
Aquaporin 4 (AQP4) channel blocker


Activators
Cat. No. Product Name / Activity
0442 4-Chlorophenylguanidine hydrochloride
ASIC3 positive allosteric modulator
5028 GMQ hydrochloride
Selective ASIC3 opener
3647 Neuropeptide SF (mouse, rat)
ASIC3 activator; neuropeptide FF receptor agonist
Blockers
Cat. No. Product Name / Activity
0890 Amiloride hydrochloride
Non-specific ASIC blocker; Na+ channel blocker
4804 APETx2
ASIC3 channel blocker
6705 Diminazene aceturate
ASIC blocker; antihyperalgesic
5042 Psalmotoxin 1
Potent and selective ASIC1a channel blocker
Others
Cat. No. Product Name / Activity
5938 Mambalgin 1
Selective ASIC1a inhibitor; analgesic


Activators
Cat. No. Product Name / Activity
1544 (±)-Bay K 8644
CaV1.x activator
1546 (S)-(-)-Bay K 8644
CaV1.x activator; (S)-(-)-enantiomer of (±)-Bay K 8644
1403 FPL 64176
Potent CaV1.x activator
2851 Nefiracetam
CaV1.x and CaV2.2 activator; cognitive enhancer
Blockers
Cat. No. Product Name / Activity
2571 Amlodipine besylate
CaV1.x blocker
1545 (R)-(+)-Bay K 8644
CaV1.x blocker; (R)-(+)-enantiomer of (±)-Bay K 8644; also TMEM176B inhibitor
2629 Cilnidipine
Dual CaV1.x and CaV2.x blocker
6170 Cinacalcet hydrochloride
CaV1.x blocker; also CaSR allosteric agonist and CYP2D2 inhibitor
0685 Diltiazem hydrochloride
CaV1.x blocker
3733 Efonidipine hydrochloride monoethanolate
CaV1.x and CaV3.x blocker
2960 Felodipine
CaV1.x blocker
6407 Fendiline Hydrochloride
CaV1.x blocker; also K-Ras inhibitor
2004 Isradipine
CaV1.x blocker
2959 Lercanidipine hydrochloride
CaV1.x blocker
0840 Loperamide hydrochloride
CaV1.x and CaV2.x blocker; also peripherally acting μ agonist
1075 Nifedipine
CaV1.x blocker
1124 (R)-(-)-Niguldipine hydrochloride
CaV1.x blocker; also α1A antagonist; less active enantiomer of (S)-(+)-Niguldipine
1123 (S)-(+)-Niguldipine hydrochloride
CaV1.x blocker; also α1A antagonist
5711 Nilvadipine
CaV1.x blocker; also Syk kinase inhibitor
0600 Nimodipine
CaV1.x blocker
0601 Nitrendipine
CaV1.x blocker
1806 SR 33805 oxalate
CaV1.x blocker; binds allosterically to distinct site
0654 Verapamil hydrochloride
CaV1.x blocker


Activators
Cat. No. Product Name / Activity
2851 Nefiracetam
CaV1.x and CaV2.2 activator; cognitive enhancer
Blockers
Cat. No. Product Name / Activity
2799 ω-Agatoxin IVA
CaV2.1 blocker
2802 ω-Agatoxin TK
CaV2.1 blocker
2629 Cilnidipine
Dual CaV1.x and CaV2.x blocker
1085 ω-Conotoxin GVIA
CaV2.2 blocker
1084 ω-Conotoxin MVIIC
CaV2.x blocker
5235 Huwentoxin XVI
Potent and reversible CaV2.2 blocker
840 Loperamide hydrochloride
CaV1.x and CaV2.x blocker; also peripherally acting μ agonist
3552 PD 173212
Potent CaV2.2 blocker
1439 Ruthenium Red
Non-selective CaV2.1 and 2.2 blocker; also blocks TRPV channels
2945 SNX 482
Potent and selective CaV2.3 blocker


Activators
Cat. No. Product Name / Activity
6239 SAK 3
Potent CaV3.1 and 3.3 activator; orally bioavailable
Blockers
Cat. No. Product Name / Activity
6770 ABT 639
CaV3.2 and CaV3.1 channel blocker; orally bioavailable
4055 L-Ascorbic acid
Selective CaV3.2 blocker
3733 Efonidipine hydrochloride monoethanolate
CaV1.x and CaV3.x blocker
0522 Flunarizine dihydrochloride
Dual CaV3.x and NaV blocker
2198 Mibefradil dihydrochloride
CaV3.x blocker
4507 ML 218 hydrochloride
CaV3.x blocker
2268 NNC 55-0396 dihydrochloride
Highly selective CaV3.x blocker
6651 (2R/S)-6-PNG
CaV3.2 blocker; active in vivo
4665 ProTx I
CaV3.1 blocker; also inhibits NaV1.8 and KV2.1
6367 Z 944
CaV3.x blocker


Blockers
Cat. No. Product Name / Activity
3934 Benidipine hydrochloride
Non-selective Cav blocker; also mineralocorticoid receptor antagonist
4117 Bepridil hydrochloride
Non-selective Ca2+ channel blocker; also NCX inhibitor
3086 L-651,582
Non-selective Ca2+ channel blocker
5470 QAQ dichloride
Photoswitchable Nav, Kv and Cav channel blocker
6179 UK 59811 hydrochloride
CaVAb blocker
Others
5948 DMNPE-4 AM-caged-calcium
Caged calcium; cell permeable
8006 Gabapentin
Selectively binds the α2δ subunit of CaV channels. Anticonvulsant
3775 Pregabalin
Anticonvulsant; selectively binds the α2δ subunit of voltage-sensitive calcium channels


Modulators
Cat. No. Product Name / Activity
6481 AP 14145 hydrochloride
KCa2 channel negative allosteric modulator
4949 MaxiPost
Potassium channel modulator; exerts subtype-specific effects
3895 NS 309
Positive modulator of KCa2 and KCa3.1 channels
4597 NS 8593 hydrochloride
Selective KCa2 (SK) channel negative modulator; inhibits SK currents
6398 SKA 121
Positive allosteric modulator of KCa3.1 channels
Activators
Cat. No. Product Name / Activity
2665 BMS 191011
Potent BKCa (KCa1.1) channel opener
2953 CyPPA
Activator of KCa2.2 and KCa2.3 channels
1422 DCEBIO
More potent analog of 1-EBIO (Cat. No. 1041). Activates hKCa3.1/Cl- conductance
1041 1-EBIO
Activator of epithelial KCa channels
4311 GW 542573X
Selective activator of KCa2.1 channels
4788 NS 11021
Activator of BKCa (KCa1.1) channels
3804 NS 1619
Activator of BKCa (KCa1.1) channels
5276 NS 19504
Activator of BKCa (KCa1.1) channels
3670 SKA 31
Activator of KCa3.1 and KCa2 channels
Blockers
Cat. No. Product Name / Activity
1652 Apamin
KCa2 channel blocker (small conductance)
1087 Charybdotoxin
KCa channel blocker (big conductance)
1086 Iberiotoxin
KCa channel blocker (big conductance)
5571 Lei-Dab 7
High affinity, selective KCa2.2 blocker
4864 NS 6180
Potent KCa3.1 channel blocker
2006 Paxilline
Potent blocker of BKCa (KCa1.1) channels
4617 Penitrem A
Potent and selective BKCa (KCa1.1) channel blocker
2946 TRAM 34
Potent and highly selective KCa3.1 channel blocker
4952 TRAM 39
Potent KCa3.1 blocker
1310 UCL 1684
Highly potent blocker of KCa2
2661 UCL 2077
Slow afterhyperpolarization (sAHP) channel blocker; sub-type selective Kv channel effects
Others
Cat. No. Product Name / Activity
5948 DMNPE-4 AM-caged-calcium
Caged calcium; cell permeable



Activators
Cat. No. Product Name / Activity
1377 Cromakalim
Kir6 (KATP) channel opener
0964 Diazoxide
Kir6 (KATP) channel opener
1378 Levcromakalim
Kir6 (KATP) channel opener; active enantiomer of cromakalim (Cat. No. 1377)
0583 Minoxidil
Kir6 channel (KATP) opener
5380 ML 297
Selective Kir3.1/3.2 (GIRK1/2) channel activator
2147 Nicorandil
Kir6 (KATP) channel opener and NO donor
1355 P1075
Potent Kir6 (KATP) channel opener
2580 Tenidap
Opener of Kir2.3. Also cyclooxygenase (COX-1) inhibitor
2076 Y-26763
Kir6 (KATP) channel opener
2077 Y-27152
Prodrug of Kir6 (KATP) channel opener Y-26763 (Cat. No. 2076); orally active in vivo
0882 ZM 226600
Kir6 (KATP) channel opener
Blockers
Cat. No. Product Name / Activity
6086 AMP PNP
Kir6 blocker; non-hydrolyzable AMP analog
3590 Gambogic acid
Kir2.1 channel blocker. Also apoptosis inducer
9011 Glibenclamide
Kir6 (KATP) channel blocker
2396 Glimepiride
Kir6 (KATP) channel blocker
4549 ML 133 hydrochloride
Kir2 channel blocker
6889 ML 418
Kir 7.1 inhibitor; also inhibits Kir 6.2
4231 Nateglinide
Kir6 (KATP) blocker; displays high affinity for SUR1/Kir6.2 channels
2095 PNU 37883 hydrochloride
Vascular Kir6 (KATP) channel blocker
3805 Repaglinide
Kir6 (KATP) channel blocker
0925 SCH 23390 hydrochloride
Kir3 channel blocker; also potent dopamine D1-like antagonist and 5-HT2C agonist
3948 Terfenadine
KV11.1 (hERG) and Kir6 (KATP) channel blocker. Also H1 antagonist
4339 Tertiapin LQ
Selective Kir1.1 blocker; derivative of tertiapin-Q (Cat. No. 1316)
1316 Tertiapin-Q
Selective blocker of inward-rectifier K+ channels
6877 VU 0134992
Kir4.1 blocker
3891 VU 590 dihydrochloride
Inhibitor of Kir1.1 (ROMK) and Kir7.1
4197 VU 591 hydrochloride
Selective Kir1.1 (ROMK) inhibitor


Modulators
Cat. No. Product Name / Activity
1540 DCPIB
Modulator of K2P channels; activates TREK1 and TRAAK, inhibits TRESK, TASK1 and TASK3; also VSAC blocker
Activators
Cat. No. Product Name / Activity
3797 BL 1249
K2P2.1 (TREK-1) and K2P10.1 (TREK-2) activator
6689 GI 530159
K2P2.1 (TREK-1) and K2P10.1 (TREK-2) channel activator
6887 ML 335
Selective K2P2.1 (TREK-1) and K2P10.1 (TREK-2) activator
6888 ML 402
Selective TREK channel activator
6886 ML 67-33
K2P2.1 (TREK-1), K2P10.1 (TREK-2) and K2P4.1 (TRAAK) channel activator
3026 ONO 1078
K2P10.1 (TREK-2) activator; also selective CysLT1 antagonist
6484 Terbinafine hydrochloride
Selective K2P9.1 (TASK-3) activator; also inhibits fungal squalene epoxidase
Blockers
Cat. No. Product Name / Activity
6972 A 1899
Potent K2P3.1 (TASK-1) and K2P9.1 (TASK-3) blocker
5337 ML 365
Potent and selective K2P3.1 (TASK-1) channel blocker
5338 PK-THPP
Potent K2P9.1 (TASK-3) channel blocker
5594 Spadin
Potent K2P2.1 (TREK-1) channel blocker


Modulators
Cat. No. Product Name / Activity
4949 MaxiPost
Potassium channel modulator; exerts subtype-specific effects
2661 UCL 2077
Sub-type selective Kv channel effects; slow afterhyperpolarization (sAHP) channel blocker
Activators
Cat. No. Product Name / Activity
2867 Flupirtine maleate
KV7 channel activator; also GABAA modulator and indirect NMDA antagonist
4305 ICA 069673
KV7.2/KV7.3 channel opener
4950 ICA 110381
KV7.2/7.3 activator; displays anticonvulsant properties
2660 L-364,373
KV7.1 channel activator, activates IKs
4519 ML 213
KV7.2 and KV7.4 channel opener
4777 ML 277
Selective KV7.1 (KCNQ1) potassium channel activator; augments IKs current
3062 NS 1643
KV11.1 (hERG) channel activator; antiarrhythmic
4462 NS 3623
KV11.1 (hERG) and KV4.3 channel activator; antiarrhythmic
4166 NS 5806
KV4.3 channel activator
2830 PD 118057
Selective KV11.1 (hERG) channel activator
5083 QO 58
Kv7 channel opener
6233 Retigabine
KV7 channel activator
Blockers
Cat. No. Product Name / Activity
4812 ADWX 1
Potent and selective KV1.3 channel blocker
5195 Agitoxin 2
Potent Shaker K+ channel blocker
0940 4-Aminopyridine
Non-selective KV channel blocker
5659 AmmTX3
KV4 channel blocker
3489 Astemizole
Potent KV11.1 (hERG) channel blocker. Also histamine H1 antagonist
6318 Azimilide dihydrochloride
Kv11.1 (hERG) channel blocker
2787 BAPTA AM
hKV11.1 (hERG), hKV1.3 and hKV1.5 channel blocker. Also Ca2+ chelator
5184 BDS I
Potent and reversible Kv3.4 potassium channel blocker; neuroprotective
5929 BeKm 1
Potent and selective KV11.1 (hERG) channel blocker
1412 Chromanol 293B
IKs blocker. Also blocks ICFTR
1475 (-)-[3R,4S]-Chromanol 293B
IKs blocker. Enantiomer of Chromanol 293B (Cat. No. 1412)
1399 CP 339818 hydrochloride
Non-peptide, potent KV1.3 channel blocker
2330 DMP 543
K+ channel blocker
3757 Dofetilide
KV11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)
2533 DPO-1
Blocker of KV1.5 channel and IKur current
1808 E-4031 dihydrochloride
KV11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)
5676 Guangxitoxin 1E
Potent Kv2.1 and Kv2.2 channel blocker
5011 HMR 1556
Potent and selective Iks channel blocker
3899 JNJ 303
Potent and selective IKs blocker
4130 KN 92
K+ channel (Kv) blocker. Inactive analog of KN 93
1278 KN 93
K+ channel blocker (KV); also inhibitor of CaM Kinase II
1999 Linopirdine dihydrochloride
KV7 (KCNQ) channel blocker
3563 Margatoxin
Potent KV1.3 channel blocker
4665 ProTx I
CaV3.1 channel blocker; also inhibits NaV1.8 and KV2.1
4367 Psora 4
Potent KV1.3 channel blocker
3220 ShK-Dap22
Extremely potent and selective KV1.3 blocker; suppresses T cell activation in vitro
3948 Terfenadine
KV11.1 (hERG) and Kir6 (KATP) channel blocker. Also H1 antagonist
3068 Tetraethylammonium chloride
Non-selective K+ channel blocker
3829 UK 78282 hydrochloride
Blocker of KV1.3 and KV1.4 channels
2000 XE 991 dihydrochloride
Potent, selective KV7 (KCNQ) channel blocker; blocks M-currents
Others
Cat. No. Product Name / Activity
5462 AAQ chloride
Photoswitchable Kv channel blocker
5858 Droperidol
hERG channel ligand; also D2 receptor antagonist
2007 Fluticasone propionate
Selective glucocorticoid agonist; KV1 potentiator
6087 Perifosine
Modulates Kv2.1current; also PKB/Akt inhibitor
5470 QAQ dichloride
Photoswitchable Nav, Kv and Cav channel blocker


Activators
Cat. No. Product Name / Activity
0464 Capsazepine
Activator of ENaCδ; also vanilloid receptor antagonist
Blockers
Cat. No. Product Name / Activity
3380 Benzamil
NCX inhibitor, Deg/ENaC channel blocker; amiloride (Cat. No. 0890) derivative
3379 Phenamil
Inhibits TRPP3-mediated currents; also inhibits epithelial Na+ channels
Others
Cat. No. Product Name / Activity
5463 PA 1 dihydrochloride
Photoswitchable ENaC blocker


Activators
Cat. No. Product Name / Activity
5941 OD1
Potent hNav1.4, rNav1.6 and rNav1.7 channel activator
2918 Veratridine
Voltage-gated Na+ channel opener
Blockers
Cat. No. Product Name / Activity
2976 A 803467
Selective NaV1.8 channel blocker
4249 A 887826
Potent voltage-dependent NaV1.8 channel blocker
2404 Ambroxol hydrochloride
Na+ channel blocker
0890 Amiloride hydrochloride
Na+ channel blocker; also I2 imidazoline ligand
6159 4,9-Anhydrotetrodotoxin
Potent and selective Nav1.6 channel blocker
4804 APETx2
NaV1.8 and NaV1.2 blocker; also blocks ASIC3 channels
4098 Carbamazepine
Inhibitor of neuronal NaV channels; anticonvulsant
2642 Co 102862
State-dependent of voltage-gated sodium channels
1470 Flecainide acetate
Cardiac Na+ channel blocker. Antiarrhythmic
0522 Flunarizine dihydrochloride
Dual Na+/Ca2+ channel (T-type) blocker
4718 Huwentoxin IV
Selective NaV1.7 channel blocker
5066 ICA 121431
Potent and selective NaV1.3 and NaV1.1 channel blocker
4913 Jingzhaotoxin III
Selective NaV1.5 channel blocker
3251 KC 12291 hydrochloride
Orally active atypical Na+ channel blocker; cardioprotective
3865 Licarbazepine
Active metabolite of oxcarbazepine (Cat. No. 3864)
3057 Lidocaine
Na+ channel blocker
2596 Mexiletine hydrochloride
Na+ channel blocker; antiarrhythmic agent
4691 NAV 26
Selective Nav1.7 channel blocker
3864 Oxcarbazepine
Anticonvulsant; inhibits Na+ channel activity
4916 PF 04885614
Potent and selective NaV1.8 channel blocker; active in vivo
5931 PF 05089771
Potent and selective Nav1.7 channel blocker
4914 Phrixotoxin 3
Potent blocker of NaV1.2, NaV1.3 and NaV1.5 channels
4665 ProTx I
CaV3.1 channel blocker; also inhibits NaV1.8 and KV2.1
4023 ProTx II
Selective NaV1.7 channel blocker
5792 ProTx III
Potent Nav1.7 blocker; analgesic
1043 QX 222
Na+ channel blocker
1014 QX 314 bromide
Na+ channel blocker
2313 QX 314 chloride
Na+ channel blocker
4029 Ralfinamide mesylate
Na+ channel blocker
0768 Riluzole hydrochloride
Na+ channel blocker; also inhibits GABA uptake and glutamate release
4044 Sipatrigine
NaV blocker; neuroprotective
4435 TC-N 1752
NaV channel blocker
1078 Tetrodotoxin
Na+ channel blocker
1069 Tetrodotoxin citrate
Na+ channel blocker; citrate salt of tetrodotoxin (Cat. No. 1078)
2815 Valproic acid, sodium salt
Blocks voltage-gated Na+ channels
0757 Vinpocetine
Na+ channel blocker
Others
Cat. No. Product Name / Activity
5184 BDS I
Attenuates inactivation of sodium currents by acting on Nav1.7 and Nav1.3 channels; neuroprotective
1539 β-Pompilidotoxin
Slows neuronal Na+ channel inactivation
5470 QAQ dichloride
Photoswitchable Nav, Kv and Cav channel blocker
3828 Rufinamide
Prolongs inactivation of sodium channels; anticonvulsant
6179 UK 59811 hydrochloride
CaVAb blocker