Potassium Channel Inhibitor

Quinidine (15% dihydroquinidine) (Standard) is the analytical standard of Quinidine (15% dihydroquinidine) (HY-B1751). This product is intended for research and analytical applications. Quinidine (15% dihydroquinidine) is an orally active antiarrhythmic agent. Quinidine (15% dihydroquinidine) reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine (15% dihydroquinidine) exerts sustained block and open-channel block effects on I_K(f). Quinidine (15% dihydroquinidine) alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine (15% dihydroquinidine) can be used in studies related to uterine sarcoma and seizures.

Cisapride (R 51619) (Standard) is the analytical standard of Cisapride (HY-14149). This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active, selective 5-HT₄ receptor agonist with an EC₅₀ of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC₅₀ of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT₄ receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis.

NS8593 hydrochloride (Standard) is the analytical standard of NS8593 (hydrochloride) (HY-110105). This product is intended for research and analytical applications. NS8593 hydrochloride is a potent and selective small conductance Ca2+-activated K+ channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a K_d value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca2+-dependently (K_ds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+), and does not affect the Ca2+-activated K+ channels of intermediate and large conductance (hIK and hBK channels, respectively).

Astemizole (Standard) is the analytical standard of Astemizole. This product is intended for research and analytical applications. Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K⁺ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects.

UK-78282 hydrochloride is a K_V1.3 channel inhibitor with an IC₅₀ value of 0.20 μM and a K_d of 0.39 μM. UK-78282 hydrochloride also inhibits the Kv1.4 Potassium Channel. UK-78282 hydrochloride blocks KV1.3 in a use-dependent manner and inhibits human T lymphocyte activation by regulating the cell cycle. UK-78282 hydrochloride can be used in research related to mental disorders, such as depression and schizophrenia.

Propafenone (Standard) is the analytical standard of Propafenone. This product is intended for research and analytical applications. Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC₅₀=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC₅₀ values of 4.9 μm and 8.6 μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.

Ac4ManNAz (Standard) is the analytical standard of Ac4ManNAz (HY-W728531). This product is intended for research and analytical applications. Ac4ManNAz can be taken up by cells and is an azide-containing metabolic glycoprotein labeling reagent that selectively modifies proteins. Commonly used for cell labeling, tracK_ing and proteomic analysis. Ac4ManNAz contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Ac4ManNAz can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.

G-479 is the inhibitor for MEK and hERG channel (IC₅₀=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC₅₀ of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats.

ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC₅₀ value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases.

Antihistamine-1 (Standard) is the analytical standard of Antihistamine-1 (HY-100238). This product is intended for research and analytical applications. Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.

VU590 (Standard) is the analytical standard of VU590 (HY-108595). This product is intended for research and analytical applications. VU590 is a potent and moderately selective ROMK (K_ir1.1) inhibitor, with an IC₅₀ of 290 nM. VU590 also inhibits K_ir7.1, with an IC₅₀ of 8 μM. VU590 is not a good probe of ROMK function in the K_idney.

CGC-11150 is a decamine-based polyamine analog that acts as a voltage-dependent pore blocker of Kir channels. CGC-11150 produces voltage-dependent pore block similar to that of Spermine (HY-B1777) in recombinant Kir6.2^{[N160D, L164C, C166S, Δ36]} + SUR1 channels, but with faster on and off rates. CGC-11150 inhibits the development of and induces regression of laser-induced choroidal neovascularization (CNV). CGC-11150 is used in studies related to choroidal neovascularization.

Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue.

DPO-1 (Standard) is the analytical standard of DPO-1 (HY-100712). This product is intended for research and analytical applications. DPO-1 is a potent Kv1.5 and Kv1.3 (EC50 = 3.1 μM) channels inhibitor with potential immunomodulatory and anti-inflammatory effects. DPO-1 reduces Kv1.3 current density, blunts Ca2+ influx in Ca2+-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. DPO-1 inhibits Uric acid sodium (HY-B2130A) (MSU)-induced NLRP3 inflammasome activation by blocking Kv1.5-mediated K+ efflux. DPO-1 can be used for the study of immunologic disorders and atrial fibrillation.

AWD 122-60 is a potassium channel blocker and calcium sensitizer, with IC₅₀ values of 11 μM and 29 μM, respectively, against mouse skeletal muscle ATP-sensitive potassium (K_ATP) channels. AWD 122-60 exerts potent positive inotropic activity. AWD 122-60 exhibits antiarrhythmic activity in vivo and prolongs myocardial refractory period in vitro. AWD 122-60 can be used for research related to arrhythmias.

Etimizol (Standard) is the analytical standard of Etimizol. This product is intended for research and analytical applications. Etimizol(Ethymisole; Antiffine; Ethylnorantifein) was shown to relieve amnesia effectively in the origin of which there is the hypoxic component (hypobaric hypoxia, actinomycin D, mechanical injury of the brain). Etimizol can decrease the K-+ permeability of neurons' membrane during action potential.

Pirmenol (hydrochloride) (Standard) is the analytical standard of Pirmenol (hydrochloride) (HY-100795A). This product is intended for research and analytical applications. Pirmenol ((±)-Pirmenol) hydrochloride is an orally active antiarrhythmic agent. Pirmenol hydrochloride inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol hydrochloride can be used in the research of cardiovascular disease, such as atrial fibrillation.

Nifekalant (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC₅₀ of 10 μM. Nifekalant can be used for refractory ventricular tachyarrhythmias research.

HMR 1556 (Standard) is the analytical standard of HMR 1556 (HY-106369). This product is intended for research and analytical applications. HMR 1556, a chromanol derivative, is a potent IKs blocker with IC₅₀s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively.

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.