Calcium Channel Inhibitor

dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca²⁺ influx with an IC₅₀ value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal.

Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Ca_vα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Ca_vα2δ-1 with a K_i of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a K_i of 383 nM and IC₅₀ of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain.

Perisulfakinin, a satiety signaling neuropeptide, inhibits the activity of central neurons promoting general activity.

Cetiedil citrate is a vasodilator and antihemolytic agent. Cetiedil citrate exerts anti-sickle cell anemia effects by blocking Ca²⁺-activated K⁺ channels (Gardos/KCa3.1). Cetiedil citrate is a muscarinic receptor antagonist that inhibits calcium-dependent release of acetylcholine (ACh) from mediated reconstituted proteoliposomes, with a K_i value of 5 μM. Cetiedil citrate possesses analgesic, spasmolytic and local anesthetic activities. Cetiedil citrate can be used in research related to ischemic leg pain caused by vascular diseases and sickle cell disease.

Cimicifugic acid D (2-Caffeoylpiscidic acid) is a benzyltartaric acid ester that induces vasodilation of precontracted rat aortic strips and endothelium-independent relaxation mechanism. Cimicifugic acid D inhibits extracellular Ca²⁺ influx through receptor-operated Ca²⁺ channels (ROC) in Norepinephrine (HY-13715)-induced contraction of rat aortic strips, without affecting voltage-dependent Ca²⁺ channels (VDC) or K⁺-induced contractions.

Cav 3.2 inhibitor 2 is a Ca_v3.2 T-type Ca²⁺ channels inhibitor with an IC₅₀ of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain.

L-Ascorbic acid (L-Ascorbate) magnesium, an electron donor, is an endogenous antioxidant. L-Ascorbic acid selectively inhibits Cav3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid is also a collagen deposition promoter and elastin production inhibitor. L-Ascorbic acid exhibits anticancer effects by generating reactive oxygen species (ROS) and selectively damaging cancer cells.

Argireline acetate (Acetyl hexapeptide-3 acetate) is a non-toxic, skin-permeable, antiwrinkle peptide. Argireline acetate significantly inhibits Ca²⁺ dependent neurotransmitter release (acetylcholine) at the neuromuscular junction. Argireline acetate has antiwrinkle and anti-aging activity.

1-Phenyl-2-propanol (Standard) is the analytical standard of 1-Phenyl-2-propanol. This product is intended for research and analytical applications. 1-Phenyl-2-propanol (Benzylmethylcarbinol) is a natural product.

KCa1.1 channel activator-1 (compound 1E), a Quercetin hybrid derivative, is a selective vascular K_Ca1.1 channel channel stimulator. KCa1.1 channel activator-1 also displays Ca_V1.2 channel blocking activity. KCa1.1 channel activator-1 exhibits weak myorelaxant activity.

Polygalasaponin F (Standard) is the analytical standard of Polygalasaponin F. This product is intended for research and analytical applications. Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca²⁺ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease.

Azimilide-d₈ (NE-10064-d₈) dihydrochloride is the deuterium labeled Azimilide dihydrochloride (HY-18600A). Azimilide dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of I_Ks (IC₅₀ = 2.6 μM (2mM [K⁺]ₑ)) and I_Kr (IC₅₀ = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC₅₀s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (I_Ca) (IC₅₀ = 17.8 μM) and sodium current (I_Na) (IC₅₀ = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation.

Gymnopusin is an L-type voltage-dependent calcium channel blocker and vasorelaxant. Gymnopusin inhibits KCl- and Norepinephrine-induced contractility as well as CaCl₂-induced contractions. Gymnopusin induces endothelium-independent relaxation involving the opening of ATP-sensitive and calcium-activated potassium channels. Gymnopusin disrupts membranes through tonoplast lysis, leading to electrolyte leakage, chlorophyll loss, and photobleaching in duckweed. Gymnopusin inhibits radicle elongation in Amaranthus hypochondriacus seedlings and exhibits phytotoxicity against duckweed. Gymnopusin shows moderate cytotoxicity against mammalian cell lines. Gymnopusin can be used for research on hypertension.

Elpetrigine (JZP 4) is a potent calcium and sodium channel blocker. Elpetrigine has anticonvulsant, antidepressant, antimania and anxiolytic effects. Elpetrigine can be used in the research of epilepsy and bipolar disorder.

FK 584 is a potent detrusor muscle contraction inhibitor. FK 584 possesses potent antimuscarinic activity and weak calcium channel blocking activity. FK 584 has demonstrated potent detrusor muscle inhibitory activity in various experimental models with a manageable risk of mydriasis. FK 584 can be used to study overactive bladder (OAB).

COX-2/CaV2.2-IN-1 is an orally active and selective dual COX-2/CaV2.2 inhibitor, exhibiting a COX-2 IC₅₀ of 0.26 μM and a CaV2.2 IC₅₀ of 0.29 μM. COX-2/CaV2.2-IN-1 suppresses inflammatory responses and inflammatory mediator (IL-6, TNF-α, NO) production. COX-2/CaV2.2-IN-1 produces pronounced analgesic effects in diverse models of inflammatory, neuropathic, and visceral pain. COX-2/CaV2.2-IN-1 can be used for the research of chronic pain.

Migrastatin is a typical Fascin1 inhibitor. Migrastatin is isolated from a cultured broth of Streptomyces sp. MK929-43F1. Migrastatin inhibits tumor cell migration.

ACS-67 is a hydrogen sulphide-releasing derivative of Latanoprost acid. ACS-67 has the potential for glaucoma research.

(S)-Verapamil-d₇ (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.

(R)-Lercanidipine hydrochloride is the R-enantiomer of Lercanidipine. (R)-lercanidipine hydrochloride is a calcium channel blocker.