ca2+ influx

D-GsMTx4 TFA belongs to natural products and is a TRPC1/6 and Piezo2 channel inhibitor with high selectivity and cell permeability, inhibiting Ca2+ influx and the mTOR pathway. This compound is used in research on myocardial infarction, chronic pain, and pulmonary fibrosis.

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.

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.

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.

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.

Yaddle1 is an agonist of the mechanically sensitive ion channel protein Piezo1, with a half-maximal effective concentration (MEC50) of 0.40 μM. It significantly induces Ca2+ influx in T cells, prompting T cell activation responses. Yaddle1 is applicable in vaccine adjuvant research.

Antiallergic agent-5 (Compound 4f) is an anti-allergy substance. It inhibits Ca2+ influx and suppresses IgE/Ag-induced release of IL-6 and TNF-α. Additionally, Antiallergic agent-5 prevents mast cell degranulation and alleviates passive cutaneous anaphylaxis in mice, while also reducing vascular leakage.

OBAA is a phospholipase inhibitor and a broad-spectrum PLA2 inhibitor. It exhibits potent anti-inflammatory activity by blocking arachidonic acid pathways, used for acute inflammation research.

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 the mitochondrial Na⁺/Ca²⁺ exchanger (mNCX) that modulates mitochondrial calcium homeostasis, and at low micromolar concentrations ITH-12575 reduces Ca²⁺ influx through CALHM1 channels, supporting its use in studies of mitochondrial signaling, neuronal excitability, calcium-dependent metabolism, and neurodegenerative disease mechanisms.

Cyclic ADP-Ribose (ammonium salt) (cADPR) is an endogenous NAD⁺ metabolite that triggers Ca²⁺ release from ER stores via ryanodine receptors and is synthesized by CD38 and CD157. It may also activate TRPM2 in a temperature-dependent manner. Showing potential in research related in inflammation and immunology.

(±)-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.