calcium ion influx

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

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. Etripamil is an antagonist of short-acting L-type calcium-channel. It has a rapid onset of action designed for intranasal administration. It is also used to treat Paroxysmal Supraventricular Tachycardia.

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 into mast cells.

Etripamil (MSP-2017) hydrochloride is a fast-acting L-type calcium channel blocker used in the study of paroxysmal supraventricular tachycardia (PSVT). By inhibiting calcium ion influx through slow calcium channels, etripamil hydrochloride slows atrioventricular nodal conduction and extends the atrioventricular nodal refractory period.

FLY26 is a selective partial antagonist of GluN2B, with an IC50 value of 0.64 μM. FLY26 inhibits the GluN2B subunit of NMDA receptors, reducing calcium ion influx and reactive oxygen species (ROS) production. It also activates the BDNF/TrkB/CREB neuroprotective signaling pathway, mitigating excitotoxicity and mitochondrial dysfunction. FLY26 holds potential for treating neurological deficits caused by cerebral ischemia-reperfusion injury.

SW016789 is a potent high-secretion inducer targeting VDAC1, which directly stimulates insulin secretion and calcium ion influx in β cells. It transiently induces endoplasmic reticulum stress (ER stress) without causing β cell death. The response it triggers is reversible and non-apoptotic, making SW016789 useful for studying β cell dysfunction in type 2 diabetes (T2DM).

Calcium Channel antagonist6 (Compound 328) is a highly selective antagonist of the voltage-gated calcium channel CaV2.2, with an IC50 of 0.37 μM. It inhibits calcium ion influx caused by neuronal depolarization and shows potential for research in neuropathic pain.

TRPA1 agonist-2 (Compound 4B) is an orally bioavailable and highly selective activator of the TRPA1 channel. It induces calcium ion influx and stimulates GLP-1 secretion. This compound shows potential for research in diabetes, obesity, and related neurodegenerative diseases.

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 downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

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.

Flufenamic Acid-D4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg/kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

Capa-2 is a neuropeptide that induces calcium ion influx and stimulates nitric oxide (NO) production, which activates soluble guanylate cyclase (sGC) and increases intracellular cGMP levels, thereby driving ion and fluid secretion. Capa-2 is utilized in diuretic research.

[DArg10, Aib20]TLQP-21, also known as a TLQP-21 analogue, functions as a C3aR partial agonist and a C3aR functional antagonist (with a β-arrestin recruitment EC50 of 854 nM). It does not exhibit significant calcium ion influx activity or enhanced adrenergic-induced lipolytic activity. This compound is applicable in research concerning inflammatory diseases, metabolic disorders, and neurological conditions.