|
T7736 |
2-Chloroadenosine
|
|
Adenosine Receptor
|
|
2-Chloroadenosine (CADO) is a metabolically stable analog of adenosine that binds to adenosine A1, A2A, and A3 receptors( Ki:300, 80, and 1,900 nM, respectively) |
|
T6777 |
Bay K 8644
|
(±)-BAY-K-8644,SQ 28,873 |
Calcium Channel
|
|
Bay K 8644 (SQ 28,873) is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM. |
|
T0370 |
Pheniramine maleate
|
Daneral,Inhiston,Trimetose |
5-HT Receptor
,
Histamine Receptor
|
|
Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived re... |
|
T40101 |
(±)-1,2-Diolein
|
1,2-Dioleoyl-rac-glycerol |
PKC
|
|
(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) (1,2-Dioleoyl-rac-glycerol) is a PKC activator. (±)-1,2-Diolein could increases myotubes Ca 2+ influx. |
|
T2711 |
Chembridge-5861528
|
TCS 5861528 |
TRP/TRPV Channel
|
|
Chembridge-5861528 (TCS 5861528) is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx with IC50 values of 14.3 and 18.7 μM, respectively. |
|
T6530 |
HC-030031
|
HC030031,TOSLAB 829227 |
TRP/TRPV Channel
|
|
HC-030031 (TOSLAB 829227) is a potent TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively. |
|
T11480 |
GSK205
|
|
Others
|
|
GSK205 is a selective TRPV4 antagonist (IC50: 4.19 μM) for inhibiting TRPV4-mediated Ca2+ influx. |
|
T12234 |
NMDA-IN-1
|
|
NMDAR
|
|
NMDA-IN-1 is a potent and NR2B-selective antagonist of NMDA(NMDA Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM). |
|
TNU0864 |
HUP30
|
|
Potassium Channel
,
Calcium Channel
|
|
HUP30 is a potent vasodilating agent. HUP30 can stimulate soluble guanylyl cyclase, activate K+ channels, and block extracellular Ca2+ influx. |
|
T11102 |
DS16570511
|
|
Calcium Channel
|
|
DS16570511 is a novel, cell-permeable inhibitor targeting the mitochondrial calcium uniporter. It effectively blocks the increase in Ca2+ influx dependent on MCU or MICU1 [1]. |
|
T5845 |
7ACC1
|
DEAC,Coumarin D 1421,7-(Diethylamino)coumarin-3-carboxylic acid,D 1421 |
Monocarboxylate transporter
|
|
7ACC1 (D 142) selectively affects a single part of the MCT symporter translocation cycle, leading to strict inhibition of lactate influx. This singular activity is associated with antitumor effects less prone to resistan... |
|
T1768 |
7ACC2
|
|
Mitochondrial Metabolism
,
Monocarboxylate transporter
|
|
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for [14C]-lactate influx; new antitumor treatment targeting lactate transport in Y cells. |
|
T16687 |
Pyr3
|
|
TRP/TRPV Channel
|
|
Pyr3 is a selective transient receptor potential canonical channel 3 inhibitor. Pyr3 inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner(IC50 = 700 nM). |
|
T1425 |
Pemirolast potassium
|
BMY 26517,TWT-8152 |
Histamine Receptor
|
|
Pemirolast Potassium is the potassium salt form of pemirolast, a pyrimidinone derivative with antiallergic property. Pemirolast potassium (TWT-8152) exerts its action by blocking the antigen-mediated calcium ion influx i... |
|
T16688 |
Pyr6
|
N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide |
TRP/TRPV Channel
|
|
Pyr6 (N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide) is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 ... |
|
T6645 |
Ropivacaine hydrochloride monohydrate
|
Ropivacaine HCl,Ropivacaine HCl monohydrate,LEA 103,LEA-103 HCl |
Potassium Channel
,
Sodium Channel
|
|
Ropivacaine hydrochloride monohydrate (LEA-103 HCl) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly. |
|
T0018 |
Procainamide hydrochloride
|
Procapan,Procainamide HCl,Pronestyl,Procanbid |
DNA Methyltransferase
,
Sodium Channel
,
AChR
,
Autophagy
|
|
Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to... |
|
T0222 |
Proparacaine hydrochloride
|
Proparacaine HCl,Proxymetacaine Hydrochloride |
Apoptosis
,
Sodium Channel
|
|
Proparacaine Hydrochloride is the hydrochloride salt form of proparacaine, a benzoic acid derivative with local anesthetic property. Proparacaine hydrochloride (Proparacaine HCl) stabilizes the neuronal membrane by bindi... |
|
T10782 |
CGP52411
|
DAPH |
EGFR
,
Beta Amyloid
|
|
CGP52411 is an orally active, and ATP-competitive inhibitor of EGFR (IC50: 0.3 μM). CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells and dramatically inhibits and reverses the formation of β-amyloid Aβ42... |
|
T16686 |
Pyr10
|
|
TRP/TRPV Channel
|
|
Pyr10 is a pyrazole derivative and a selective TRP cation 3 inhibitor. Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels. Pyr10 inhibits... |
|
T0468 |
Lidocaine
|
Lignocaine,Alphacaine,Xylocaine |
Apoptosis
,
ERK
,
NF-κB
,
MEK
,
Sodium Channel
,
Histamine Receptor
|
|
Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammat... |
|
T15257 |
Etripamil
|
MSP-2017,(-)-MSP-2017 |
Calcium Channel
|
|
Etripamil (MSP-2017) displays atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells... |
|
T1435 |
Praziquantel
|
Pyquiton,Droncit,Biltricide |
Calcium Channel
,
Antibiotic
,
Parasite
|
|
Praziquantel (Droncit) increases the permeability of the tegument of susceptible worms, resulting in an influx and increase in intra-tegumental calcium leading to rapid contractions and paralysis of the worm's musculatur... |
|
T1613 |
Hydralazine hydrochloride
|
Hydralazine HCl,Apresoline |
MAO
,
HIF/HIF Prolyl-Hydroxylase
|
|
Hydralazine hydrochloride (Apresoline) is the hydrochloride salt of hydralazine, a phthalazine derivative with antihypertensive and potential antineoplastic activities. Hydralazine alters intracellular calcium release an... |
|
TP1910L1 |
CALP1 acetate
|
CALP1 acetate(145224-99-3 free base) |
CaMK
|
|
CALP1 acetate is a calmodulin (CaM) agonist (Kd of 88 µM) that binds to the CaM EF-hand/Ca2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) by inhibiting the open of calcium channel. CALP1 blo... |
|
T1146 |
Nifedipine
|
BAY-a-1040,Procardia XL,Procardia,Adalat |
CaMK
,
Potassium Channel
,
Calcium Channel
,
Autophagy
|
|
Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation ... |
|
T22043 |
BCATc Inhibitor 2
|
|
Others
|
|
BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake,... |
|
T3979 |
Emedastine
|
LY188695,Emadine |
Histamine Receptor
|
|
Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its... |
|
T5148 |
Atosiban acetate
|
RW22164,Atosiban acetate (90779-69-4 free base),RWJ22164 |
Oxytocin Receptor
,
Vasopressin Receptor
|
|
Atosiban acetate (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban acetate (RW22164) inhibits... |
|
T4316 |
ML365
|
|
Potassium Channel
|
|
ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3). |
|
T68742 |
Inamrinone lactate
|
|
|
|
Inamrinone lactate is a positive inotropic cardiotonic with vasodilator properties, phosphodiesterase inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell. |
|
T27639 |
ITH-12575
|
|
|
|
ITH-12575 is an inhibitor of Mitochondrial Na+/Ca2+ exchange (mNCX). ITH12575 reduces Ca(2+) influx through CALHM1 at low micromolar concentrations. |
|
T26376 |
11-deoxy-PGF2a
|
11-deoxyPGF2a,11-deoxy PGF2a |
|
|
11-deoxy-PGF2a, a selective activator of TREK-2 channels, stimulates DRG c-fiber nociceptor K2P currents and limits calcium influx. |
|
T71735 |
AAL1
|
|
|
|
AAL1 is an inhibitor of dark-grown Arabidopsis thaliana seedlings, functioning through auxin receptor Transport Inhibitor Response1 (TIR1) and depending on auxin influx and efflux carriers. |
|
T14829 |
Bromoenol lactone
|
(6E)-Bromoenol lactone |
Phospholipase
|
|
Bromoenol lactone is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β; IC50: ~7 μM). It inhibits antigen-stimulated mast cell exocytosis without blocking Ca2+ infl... |
|
T68361 |
Asocainol hydrochloride
|
|
|
|
Asocainol hydrochloride ia an antiarrhythmic drug which inhibits slow Ca2+ influx. This is accompanied by alterations in normal Na+-carried action potentials. Therefore, Asocainol not only inhibits Ca2+ inflow but also i... |
|
T61438 |
Propiverine
|
|
|
|
Propiverine is a potent antimuscarinic agent that effectively inhibits cellular calcium influx, leading to the reduction of muscle spasm. It exhibits neurotropic and musculotropic effects specifically on the smooth muscl... |
|
T37760 |
Fura-2 (sodium salt)
|
|
|
|
Fura-2 is a ratiometric fluorescent calcium indicator that can be used to detect calcium in cells. It is a pentacarboxylate that displays excitation maxima of 340 and 380 nm at high and low calcium concentrations, respec... |
|
T37763 |
BTD
|
|
|
|
Selective TRPC5 activator (EC50 = 1.4 μM in a calcium influx assay, 1.3 μM in whole cell patch clamp assay). Displays >14.5-fold selectivity for TRPC5 over other TRP channels (EC50 = 20.6 μM for TRPM8). Also activates TR... |
|
T80441 |
FS-2
|
|
Calcium Channel
|
|
FS-2 is a potent, specific inhibitor of L-type CaV channels, effectively impeding high K+ or glucose-induced L-type Ca2+ influx in RIN beta cells [1]. |
|
T40750 |
12,14-Dichlorodehydroabietic acid
|
|
|
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, exhibits potent calcium-activated potassium (BK) channel opening activity. It effectively inhibits GABA-dependent chloride influx in the mammalian brain, funct... |
|
T37759 |
Fura-2 (potassium salt)
|
|
|
|
Fura-2 is a ratiometric fluorescent calcium indicator that can be used to detect calcium in cells. [1] It is a pentacarboxylate that displays excitation maxima of 340 and 380 nm at high and low calcium concentrations, re... |
|
T70224 |
Bupivacaine tartrate
|
|
|
|
Bupivacaine is a BK/SK, Kv1, Kv3, TASK-2 K Channel and voltage-gated Na channel blocker used as an anesthetic. It maybe neurotoxic at high does, inducing apoptosis in neuroblastoma cells. It acts by binding to the intra... |
|
T62660 |
MLN3126
|
|
|
|
MLN3126 is an orally active, potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis in mouse primary thymocytes with an IC50 value of 6.3 nM for calcium influx inhibition. |
|
T23102 |
OBAA
|
|
Others
|
|
OBAA is a potent inhibitor of phospholipase A2 (PLA2) with an IC 50 of 70 nM. OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei with an IC 50 of 0.4 μM [1] [2] [3]. |
|
T61475 |
Ropivacaine mesylate
|
|
|
|
Ropivacaine mesylate, a long-acting amide local anaesthetic, is used for spinal block and effectively mitigates neuropathic pain. It achieves analgesia by reversibly inhibiting sodium ion influx in nerve fibers, thus blo... |
|
T37058 |
D-myo-Inositol-1,3,4,5-tetraphosphate (sodium salt)
|
|
|
|
D-myo-Inositol-1,3,4,5-tetraphosphate (Ins(1,3,4,5)-P4) is formed by the phosphorylation of Ins(1,4,5)P3 by inositol 1,4,5-triphosphate 3-kinase. Ins(1,3,4,5)-P4 increases intracellular calcium levels by two distinct mec... |
|
T26447 |
A 78773
|
A78773,A-78773 |
|
|
A 78773 is a potent, selective, direct, and reversible 5-lipoxygenase inhibitor. It has activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tis... |
|
T79618 |
M3/PDE4 modulator-1
|
|
|
|
M3/PDE4 Modulator-1 (compound 10f) serves as a bifunctional entity functioning both as an M3 mAChR antagonist and a PDE4 inhibitor. When administered intravenously at concentrations ranging from 10 to 1000 nM/kg, this co... |
|
T69975 |
Istaroxime oxalate
|
|
|
|
Istaroxime, also known as PST-2744, is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase). Na+/K+ ATPase inhibition increases intracellular... |
