ca2+ influx

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 relaxing factor, nitric oxide.

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 fibril aggregates. CGP52411 can be used in studies about Alzheimer's diseases.

Addition of the Rhamnose (6-Deoxy-L-mannose)-rich polysaccharide, RROP-1, to normal human dermal fibroblasts (NHDFs) and human endothelial cells produced a dose-dependent stimulation of the calcium-signaling pathway, inducing fast and transient increases in Ca2 influx and intracellular free Ca2 level.

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.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

NMDA-IN-1 is a potent and NR2B-selective antagonist of NMDA, with an NMDA Ki of 0.85 nM and an NR2B Ca2+ influx IC50 of 9.7 nM.

HUP30 is a potent vasodilating agent. HUP30 can stimulate soluble guanylyl cyclase, activate K+ channels, and block extracellular Ca2+ influx.

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].

Pyr10 is a pyrazole derivative and a selective TRP cation 3 inhibitor that distinguishes between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells (IC50: 0.72 μM) and has an IC50 of 13.08 μM for store-operated Ca2+ entry in BRL-2H3 cells.

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).

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 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.

D-myo-Inositol-1,3,4,5-tetrakisphosphate potassium enhances extracellular calcium (Ca2+) influx by upregulating voltage-gated calcium channels.

SKP-451 is an ATP-sensitive potassium (K+) channel agonist. It activates ATP-sensitive K+ channels, promoting the efflux of K+, leading to membrane hyperpolarization and inhibiting Ca2+ influx, which results in the relaxation of vascular smooth muscle. SKP-451 relaxes canine coronary arteries, rabbit basilar arteries, and vertebral arteries. Additionally, SKP-451 lowers mean arterial blood pressure in conscious spontaneously hypertensive rats (SHR). It holds potential for cardiovascular disease research.

U-44069 serinol amide is a derivative of U-44069 and serves as a stable analogue of the endoperoxide, Prostaglandin H2. It functions as a vasoconstrictor, capable of inducing calcium (Ca2+) influx in preglomerular vessels.

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].

A-80b is a synthesized pyridazino[4,5-b]indole derivate with potent and long-lasting antihypertensive activity. The decrease in diastolic pressure was greater than the decrease in systolic pressure and cardiac frequency was not modified significantly. A-8

Chembridge-5861528 (TCS 5861528) is a TRPA1 channel blocker that inhibits AITC- and 4-HNE-induced calcium influx with IC50 values of 14.3 μM and 18.7 μM, respectively.

ITH-12575 is an inhibitor of Mitochondrial Na+/Ca2+ exchange (mNCX). ITH12575 reduces Ca(2+) influx through CALHM1 at low micromolar concentrations.

Cyclic ADP-ribose (cADP-ribose) is an endogenous metabolite of NAD+ that mobilizes the release of stored Ca2+ in the endoplasmic reticulum via ryanodine receptors in various cell types.[1],[2],[3],[4],[5] This second messenger is generated via the cADP-ribose synthases CD38 and CD157.[6],[5],[7] cADP-Ribose may also trigger the cell surface Ca2+ influx channel TRPM2 in a temperature-dependent manner.[8] In vitro, cADP-ribose modulates Ca2+ signaling in rat and mouse cardiomyocytes treated with isoproterenol , and treatment with this metabolite at 100 μM under heat stress conditions induces the release of oxytocin from the mouse hypothalamus.[9],[4]

(±)-1,2-Diolein [1,2-Dioleoyl-rac-glycerol] is a PKC activator that can increase Ca²⁺ influx in myotubes.

1-Stearoyl-2-arachidonoyl-sn-glycerol (DAG) is a diacylglycerol (DAG) substrate that can be hydrolyzed to 2-arachidonic acid glycerol. 1-Stearoyl-2-arachidonoyl-sn-glycerol activates PKC, induces Ca2+ influx, and can induce tracheal smooth muscle contraction.

Atosiban (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 inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

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 the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban acetate (RW22164) suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

Bay K 8644 (SQ 28,873) is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.