10 Results for "

calcium channel binding sites

" in MedChemExpress (MCE) Product Catalog:
Products (10)

10 Results for "calcium channel binding sites" in MCE Product Catalog:

3
3 Cited Publications
Cat. No.: HY-P1077
CAS No.: 145224-99-3
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity .
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3
3 Cited Publications
Cat. No.: HY-P1077A
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity .
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Cat. No.: HY-P1636
CAS No.: 113274-56-9
Research Areas:  

Metabolic Disease

Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-type calcium channels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis .
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Cat. No.: HY-101390D
CAS No.: 120054-86-6
Target:  

Calcium Channel

Research Areas:  

Cardiovascular Disease

(R)-Niguldipine, a R-epimer of Niguldipine (HY-101390B), is a calcium channel antagonist. (R)-Niguldipine exerts a vasodilatory effect by blocking calcium channels and reducing the transmembrane influx of calcium ions. (R)-Niguldipine can inhibit U-46619 (HY-108566)-induced coronary artery contraction in guinea pig Langendorff hearts (pID50 of 9.93), has high affinity for calcium channel binding sites on guinea pig skeletal muscle membranes (Ki of 8.10), and lowers blood pressure in spontaneously hypertensive rats (pED30 of 5.55). (R)-Niguldipine can improve cardiovascular diseases such as hypertension, angina pectoris, and arrhythmias .
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Cat. No.: HY-167203
CAS No.: 195991-49-2
Target:  

Calcium Channel

Research Areas:  

Cardiovascular Disease

AJG049 free base is a calcium channel (Ca 2+ channel) antagonist. AJG049 free base regulates vascular relaxation, reduces cardiac load, and improves cardiac perfusion by binding to the binding site of L-type calcium channels, specifically Diltiazem (HY-B0632). AJG049 free base can be used in cardiovascular disease research .
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Cat. No.: HY-101390A
CAS No.: 113145-70-3
Synonyms: (R)-Niguldipine hydrochloride
Target:  

Calcium Channel

Research Areas:  

Cardiovascular Disease

(-)-Niguldipine ((R)-Niguldipine) hydrochloride is a calcium channel antagonist. (-)-Niguldipine hydrochloride exerts a vasodilatory effect by blocking calcium channels and reducing the transmembrane influx of calcium ions. (-)-Niguldipine can inhibit U-46619 (HY-108566)-induced coronary artery contraction in guinea pig Langendorff hearts (pID50 of 9.93), has high affinity for calcium channel binding sites on guinea pig skeletal muscle membranes (Ki of 8.10), and lowers blood pressure in spontaneously hypertensive rats (pED30 of 5.55). (-)-Niguldipine hydrochloride can improve cardiovascular diseases such as hypertension, angina pectoris, and arrhythmias .
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Cat. No.: HY-187585
CAS No.: 104639-01-2
Fourphit is a dopamine transporter (DAT) inhibitor and phencyclidine (PCP) receptor binding agent. Fourphit irreversibly acylates the DAT [ 3H]methylphenidate binding site, reversibly binds to the PCP receptor, and sensitizes neuronal L-type DHP calcium channels. Fourphit attenuates K +-stimulated 45Ca 2+ uptake at high concentrations, and after its pretreatment, Nifedipine (HY-B0284) effectively inhibits this uptake without affecting resting calcium uptake. Fourphit reduces cocaine-induced hyperactivity, decreases cocaine-induced rearing frequency, enhances cocaine-induced thigmotaxis, elicits an acute increase in locomotor activity, and suppresses dark-cycle activity. Fourphit is used in research related to cocaine abuse and addiction .
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Cat. No.: HY-L166
1,751 compounds

Ion channel is a membrane-binding enzyme whose catalytic site is an ion conduction pore, which is opened and closed in response to specific environmental stimuli (voltage, ligand concentration, membrane tension, temperature, etc.). Ion channel provide pores for the passive diffusion of ions on the biofilm. Due to their high selectivity for ion, ion channel are generally classified as sodium (Na+ ), potassium (K+ ), calcium (Ca2+ ), chloride (Cl- ), and non-specific cation channel. Ion channel is an important contributor to cell signal transduction and homeostasis. In addition to electrical signal transduction, ion channel also have many functions: regulating vascular smooth muscle contraction, maintaining normal cell volume, regulating glandular secretion, protein kinase activation, etc. Therefore, dysfunction of ion channel can lead to many diseases, and its mechanism research is particularly important.

MCE designs a unique collection of 1,751 small molecules related to ion channel, mainly targeting Na+ channel, K+ channel, Ca2+ channel, GABA receptor, iGluR, etc. It is an essential tool for research of cardiovascular diseases, Nervous system diseases and other diseases.

Cat. No.: HY-131507
CAS No.: 3614-30-0
Target:  

mAChR

Research Areas:  

Metabolic Disease

Emepronium bromide is an antispasmodic agent for the bladder and a muscarinic receptor ligand, with an IC50 of 236 nM. Emepronium bromide is applicable to research related to bladder diseases .
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Cat. No.: HY-187618
CAS No.: 1508276-29-6
Target:  

TRP Channel

Research Areas:  

Metabolic Disease

GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx .GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity .GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses .GRC-17536 exhibits antitussive activity .GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study .GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough .
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