Search Result

Isoforms Recommended:	L-type calcium channel T-type calcium channel

Results for "

CaV1.2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Calcium Channel (21) Angiotensin Receptor (1) Apoptosis (1) Arrestin (1) COX (1) Dipeptidyl Peptidase (1) Endogenous Metabolite (1) Interleukin Related (1) Isotope-Labeled Compounds (5) Mineralocorticoid Receptor (1) NO Synthase (2) P-glycoprotein (1) P2Y Receptor (1) Potassium Channel (3) Reactive Oxygen Species (ROS) (5) Reference Standards (3) Small Interfering RNA (siRNA) (2) Sodium Channel (1) Somatostatin Receptor (1) TGF-beta/Smad (1) TNF Receptor (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (17) Inflammation/Immunology (4) Metabolic Disease (2) Neurological Disease (7)
Oligonucleotides:	Mouse Pre-designed siRNA Sets (1) Human Pre-designed siRNA Sets (1) siRNAs (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Oligonucleotides

Targets Recommended: Calcium Channel CRAC Channel Na+/Ca2+ Exchanger CaSR Calmodulin CaMK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112499

Menaquinone-7 3 Publications Verification Vitamin K2-7; Vitamin K2(35); Vitamin MK-7	TGF-beta/Smad	Cardiovascular Disease
Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS) .

HY-N2488

Demethylsuberosin 4 Publications Verification 7-Demethylsuberosin	Calcium Channel NO Synthase	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Demethylsuberosin (7-Demethylsuberosin) is a coumarin compound found in Angelica gigas Nakai. Demethylsuberosin exerts antihypertensive effects by inhibiting the L-type Ca_V1.2 channel. Demethylsuberosin has antioxidant and anti-inflammatory activities. Demethylsuberosin also exhibits neuroprotective activities against glutamate-induced toxicity in primary cultured rat cortical cells .

HY-134542

CaV1.3 antagonist-1	Calcium Channel	Neurological Disease
CaV1.3 antagonist-1 is a potent and highly selective Ca_V1.3 L-type calcium channel (LTCC) antagonist with an IC₅₀ of 1.7 μM. CaV1.3 antagonist-1 inhibits Ca_V1.3 LTCC >600-fold more potently than Ca_V1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research .

HY-106454

N-Desalkylflurazepam Norfludiazepam	Calcium Channel	Neurological Disease
N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC₅₀ values of 55 μM and 37 μM for *Ca_v1.2* and *Ca_v1.3*, respectively .

HY-P3269

Calciseptine	Calcium Channel	Cardiovascular Disease
Calciseptine is a natural polypeptide toxin found in the venom of the black mamba snake (Dendroaspis p. polylepis). Calciseptine is a highly effective and selective blocker of the L-type channel of the *Cav1.2* subtype, with an IC₅₀ value of 92 nM. Calciseptine has no effect on Cav3.1, Cav2.2, Cav2.1, Cav1.1, voltage-sensitive sodium channels and potassium channels. Calciseptine exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine can be used for research on cardiovascular diseases_[1].

HY-112499R

Menaquinone-7 (Standard) 3 Publications Verification Vitamin K2-7(Standard); Vitamin K2(35)(Standard); Vitamin MK-7 (Standard)	Endogenous Metabolite Reference Standards	Cardiovascular Disease
Menaquinone-7 (Standard) is the analytical standard of Menaquinone-7. This product is intended for research and analytical applications. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS) .

HY-Z7760

Felodipine 3,5-dimethyl ester	Mineralocorticoid Receptor	Metabolic Disease
Felodipine 3,5-Dimethyl Ester is a aryldihydropyridine derivatives for use as mineralocorticoid receptor modulator and voltage-dependent L-type calcium channel CaV1.2 inhibitor .

HY-175226

DPP8/9-IN-2	Dipeptidyl Peptidase Calcium Channel Sodium Channel Potassium Channel	Cancer
DPP8/9-IN-2 (Compound 21) is a DPP8/9 inhibitor with IC₅₀ values of 0.22 nM and 3 nM, respectively, and K_i values of 2.9 nM and 6 nM, respectively . DPP8/9-IN-2 has certain cardiotoxicity, with IC₅₀ values of 0.7 μM, 29.0 μM and 27.7 μM for hERG potassium channel, Nav1.5 sodium channel and *Cav1.2* calcium channel, respectively. DPP8/9-IN-2 can be used in the research of diseases such as tumors .

HY-126336

HM12	Calcium Channel	Cardiovascular Disease Neurological Disease
HM12 is a covalent inhibitor of L-/T-type calcium channels. HM12 can strongly inhibit the *Cav1.2* (L-type) and *Cav3.2* (T-type) calcium channels, and has selectivity for the N-type channels. HM12 produces an irreversible inhibition that persisted after washout. HM12 can be used to study diseases such as hypertension, pain, epilepsy, etc .

HY-Z15823

(R)-Verapamil Dexverapamil	Calcium Channel Potassium Channel Somatostatin Receptor Arrestin Apoptosis P-glycoprotein	Metabolic Disease Inflammation/Immunology
(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-type calcium channels (Ca_v1.2) (IC₅₀ > 300 μM), and its IC₅₀ for sodium channels (sodium channel) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC₅₀ of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp) .

HY-106454R

N-Desalkylflurazepam (Standard) Norfludiazepam (Standard)	Reference Standards Calcium Channel	Neurological Disease
N-Desalkylflurazepam (Standard) is the analytical standard of N-Desalkylflurazepam. This product is intended for research and analytical applications. N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .

HY-118202A

(-)-Gallopamil hydrochloride (-)-Methoxyverapamil hydrochloride	Calcium Channel	Cardiovascular Disease
(-)-Gallopamil (hydrochloride) exerts a selective modulation of the fast voltage-dependent inactivation. (-)-Gallopamil (hydrochloride) inhibits efficiently *Cav1.2* constructs formed by β-subunits (promoting fast voltage-dependent inactivation). (-)-Gallopamil (hydrochloride) also accelerates the voltage-dependent phase of I_Ca decay (as well as the voltage-dependent decay of Ba ²⁺ currents). (-)-Gallopamil (hydrochloride) is promising for research of antiarrhythmics .

HY-118202

(-)-Gallopamil (-)-Methoxyverapamil	Calcium Channel	Cardiovascular Disease
(-)-Gallopamil exerts a selective modulation of the fast voltage-dependent inactivation. (-)-Gallopamil inhibits efficiently *Cav1.2* constructs formed by β-subunits (promoting fast voltage-dependent inactivation). (-)-Gallopamil also accelerates the voltage-dependent phase of I_Ca decay (as well as the voltage-dependent decay of Ba ²⁺ currents). (-)-Gallopamil is promising for research of antiarrhythmics .

HY-116307

2-Thio-UTP	P2Y Receptor	Cardiovascular Disease
2-Thio-UTP is a selective P2Y₂ inhibitor with an EC₅₀ value of 50 nM. 2-Thio-UTP reduces pro-fibrotic gene expression and protein α-smooth muscle actin. 2-Thio-UTP has the potential for the research of calcific aortic valve stenosis (CAVS) .

HY-17402S

Nisoldipine-d6 BAY-k 5552-d₆	Isotope-Labeled Compounds Calcium Channel Reactive Oxygen Species (ROS)	Cardiovascular Disease
Nisoldipine-d₆ is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.

HY-17402R

Nisoldipine (Standard) BAY-k 5552 (Standard)	Reference Standards Calcium Channel Reactive Oxygen Species (ROS)	Cardiovascular Disease
Nisoldipine (Standard) is the analytical standard of Nisoldipine. This product is intended for research and analytical applications. Nisoldipine (BAY-k 5552; Sular) is a highly efficient and specific L-type Cav1.2 channel blocker with an IC50 of 10 nM.

HY-17402S3

Nisoldipine-d3 BAY-k 5552-d₃	Calcium Channel Reactive Oxygen Species (ROS) Isotope-Labeled Compounds	Cardiovascular Disease
Nisoldipine-d₃ is deuterated labeled Nisoldipine (HY-17402). Nisoldipine (BAY-k 5552; Sular) is a highly efficient and specific L-type Cav1.2 channel blocker with an IC50 of 10 nM.

HY-17402S2

Nisoldipine-d7	Isotope-Labeled Compounds Calcium Channel Reactive Oxygen Species (ROS)	Cardiovascular Disease
Nisoldipine-d₇ (BAY-k 5552-d₇) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC₅₀ of 10 nM .

HY-17402S1

Nisoldipine-d4	Isotope-Labeled Compounds Calcium Channel Reactive Oxygen Species (ROS)	Cardiovascular Disease
Nisoldipine-d₄ (BAY-k 5552-d₄) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC₅₀ of 10 nM .

HY-W701464

N-Desalkylflurazepam-d4	Isotope-Labeled Compounds	Others
N-Desalkylflurazepam-d₄ is a deuterated labeled N-Desalkylflurazepam (HY-106454). N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC₅₀ values of 55 μM and 37 μM for *Ca_v1.2* and *Ca_v1.3*, respectively .

HY-159090

AT1R antagonist 3	Calcium Channel Angiotensin Receptor	Cardiovascular Disease
AT1R antagonist 3 (Compound 1) is an antagonist for angiotensin II type 1 receptor (AT1R) and an inhibitor for calcium channel type-L CaV_1.2 (IC₅₀=0.57 μM). AT1R antagonist 3 exhibits vasodilation efficacy in solated rat aorta (10 μM, 88.7%) and antihypertensive efficacy in rat models .

HY-146173

KCa1.1 channel activator-1	Potassium Channel Calcium Channel	Cardiovascular Disease
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 .

HY-RS21233

Cacna1c Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Cacna1c Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cacna1c gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cacna1c Mouse Pre-designed siRNA Set A Cacna1c Mouse Pre-designed siRNA Set A

HY-RS01793

CACNA1C Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
CACNA1C Human Pre-designed siRNA Set A contains three designed siRNAs for CACNA1C gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CACNA1C Human Pre-designed siRNA Set A CACNA1C Human Pre-designed siRNA Set A

HY-P3269A

Calciseptine TFA	Calcium Channel	Cardiovascular Disease
Calciseptine TFA, a polypeptide found in black mamba venom, is a selcetive *Cav1.2* L-type calcium channel inhibitor with an IC₅₀ of 92 nM. Calciseptine TFA binds to the pore domain shoulder at repeats III and IV of Cav1.2, stabilizing an inactivated conformation. Calciseptine TFA exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine TFA can be used for the research of cardiovascular diseases .

HY-156889

Cav 3.1 blocker 1	Calcium Channel	Neurological Disease
Cav 3.1 blocker 1 (compound 12) is a T-type calcium channel blocker with an IC₅₀value of 160 nM for Cav3.1. Cav 3.1 blocker 1 weakly inhibits Cav 3.2 (IC₅₀ of 5000 nM), and shows no inhibition on Cav 3.3 and Cav 1.2 (IC₅₀ of >10000 nM) .

HY-175395

Onychocin B	Calcium Channel	Cardiovascular Disease
Onychocin B is a cyclic tetrapeptide isolated from Onychocola sclerotica. Onychocin B is a calcium channel blocker with an IC₅₀ of 7.1 μM for Cav1.2 .

HY-181755

Phenylaminojuglone AJ-2	NO Synthase	Inflammation/Immunology
Phenylaminojuglone AJ-2 is a nitric oxide synthase inhibitor that interacts with soluble guanylate cyclase, β-adrenergic receptor, *CaV1.2* calcium channel, KV channel and KCa channel. Phenylaminojuglone AJ-2 blocks extracellular Ca ²⁺ influx, regulates the activity of the NO−sGC−cGMP signaling pathway, and inhibits pharmacologic and electromechanical contractions of smooth muscle. Phenylaminojuglone AJ-2 is applicable to studies related to intestinal spasm .

HY-181612

*COX-2/CaV2.2-IN-1*	COX Calcium Channel Interleukin Related TNF Receptor	Neurological Disease Inflammation/Immunology
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 .

Cat. No.	Product Name

HY-L923

Ion Channel Lead-like Compound Library	9000 compounds
Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields. MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

Ion Channel Lead-like Compound Library

9000 compounds

Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields.

MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

Cat. No.	Product Name	Target	Research Area