Calcium Channel Inhibitor

Cav 3.2 inhibitor 4 (compound 21) is a potent, peripherally restricted, selective T-type calcium channel (Ca_v3.2) inhibitor, with an IC₅₀ of 0.6 μM. Cav 3.2 inhibitor 4 can be used for the research of atrial fibrillation.

wt hMLN is a microprotein that inhibits of SR Ca²⁺ pump (SERCA). wt hMLN plays an important role in skeletal muscle calcium homeostasis.

Lercanidipine-¹³C,d₃-1 (hydrochloride) is deuterium labeled Lercanidipine (hydrochloride). Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect.

Calcicludine is a protein toxin from the venom of the green mamba that inhibits high-voltage-activated calcium channel, especially L-type calcium channel.

Elgodipine (IQB-875 free base) is an orally active dihydropyridine calcium antagonist and an antianginal compound. Elgodipine inhibits both T- and L-type calcium channels (IC₅₀: 32 and 2.3 nM). Elgodipine lowers systemic vascular resistance and improves systolic cardiac function.

Norverapamil-d₇ is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

1-Octanol (Standard) is the analytical standard of 1-Octanol. This product is intended for research and analytical applications. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC₅₀ of 4 μM for native T-currents. 1-Octanol is a highly attractive biofuel with diesel-like properties.

Belfosdil is an orally active and highly specific calcium channel blocker that also inhibits the activity of acyl coenzyme A cholesterol acyltransferase.

Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.

Cd1a is a β-toxin derived from the African spider Ceratogyrus darlingi. Cd1a can regulate calcium ion channels. Cd1a inhibits human calcium ion channels (Ca_v2.2)(IC₅₀2.6 μM) and mouse sodium ion channels (Na_v1.7). Cd1a can be used in the development of peripheral pain treatment drugs .

ANO61 is a dibenzyl formamide derivative, which exhibits an antiplatelet efficacy through modulation of thrombin-induced Ca²⁺ response with an IC₅₀ of 47.7 μM.

Gabapentin-d4 hydrochloride is the deuterium labeled Gabapentin hydrochloride (HY-A0057A). Gabapentin hydrochloride is a potent, orally active P/Q type Ca²⁺ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca²⁺ influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain.

Wy 27569 is an orally active vascular selective calcium channel blocker that can effectively lower blood pressure. Wy 27569 is a thromboxane synthase inhibitor that can reshape prostaglandin balance, reduce pro thrombotic TXA2, and increase anti thrombotic PGI2. Wy 27569 can be used for research on cardiovascular diseases such as hypertension and angina.

Cavα2δ1&NET-IN-2 (Compound 45CS) 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-2 inhibits Ca_vα2δ-1 with a K_i of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a K_i of 59 nM and IC₅₀ of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain.

Clonixin-¹³C,d₃ (SCH-10304-¹³C,d₃) is the deuterium and ¹³C-labeled Clonixin (HY-121235). Clonixin is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca²⁺ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain.

Vincapusine is an inhibitor of CaV3.1 calcium channel, with a IC₅₀ of 11.83 μM against the human target. Vincapusine suppresses the functional activity of the CaV3.1 calcium channel. Vincapusine exerts antihypertensive activity by inhibiting the CaV3.1 calcium channel. Vincapusine is used in hypertension-related research.

HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models.

(2-Chlorophenyl)diphenylmethanol (Standard) is the analytical standard of (2-Chlorophenyl)diphenylmethanol. This product is intended for research and analytical applications. (2-Chlorophenyl)diphenylmethanol (UCL 1880) is an analog of the metabolite 2-chlorophen-diphenyl-methanol (CBM) of 2-chlorophenyl, The IC50 for sI(AHP) inhibition is 1-2 μM. (2-chlorophenyl)diphenylmethanol is a weak Ca2+ channel blocker.

Bupivacaine (hydrochloride monohydrate) (Standard) is the analytical standard of Bupivacaine (hydrochloride monohydrate). This product is intended for research and analytical applications. Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain.

Pinaverium bromide-d₄ is deuterium labeled Pinaverium bromide. Pinaverium bromide is an L-type calcium channel blocker with selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients.