ca2+ channel antagonist

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.

Monatepil 2maleate is an orally active Ca2+-channel antagonist and ACAT inhibitor with alpha(1)-adrenergic receptor blocking activity and antiarrhythmic properties that inhibit vasoconstriction.Monatepil 2maleate may be used to study atherosclerosis.

SR33805 is a potent antagonist of Ca2+ channel(EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively)

Blocks CaVAb, a site-directed mutant of bacterial NaVAb with full voltage-dependent Ca2+ channel function (IC50 = 194 nM). Tang et al (2016) Structural basis for inhibition of a voltage-gated Ca2+ channel by Ca2+ antagonist drugs. Nature 537 117 PMID:27556947

Calcium Channel antagonist 2 is a calcium channel antagonist (IC50=5-20 μM) that can be used to study diseases due to Ca2+ channels like pain and diabetes.

SA 2572 is a newly synthesized Ca2+ antagonist having a inhibitory effect on the fast Na+ inward channel.

Ro 23-7014, a new thiazepinone Ca2+ channel antagonist, has high affinity for peripheral (Type A) receptors.

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+ flux and [chemotaxis] CTX at 40 nM and 70 nM, respectively.

Fasudil mesylate (HA-1077; AT877) is a nonspecific, orally active inhibitor of RhoA ROCK, exhibiting additional inhibitory effects on protein kinases with a K i of 0.33 μM for ROCK1. It shows IC 50 values of 0.158 μM for ROCK2, and 4.58 μM, 12.30 μM, and 1.650 μM for PKA, PKC, and PKG, respectively. Furthermore, Fasudil mesylate acts as a potent Ca 2+ channel antagonist and vasodilator, enhancing its pharmacological profile [1] [2] [3] [4] [5] [6].

TTA-Q6, a selective T-type Ca2+ channel antagonist, exhibits potential antitumor and immunomodulatory activities for treating neurological disorders by inhibiting the uptake of extracellular calcium ions by tumor cells, thereby inducing intracellular calcium deficiency and endoplasmic reticulum (ER) stress.

Semotiadil recemate fumarate, the recemate of Semotiadil fumarate, is a novel antagonist of vasoselective Ca2+ channel.

SB 201823-A is a Ca2+ channel antagonist.

Niguldipine is a calcium channel antagonist. Niguldipine shows high affinity to Ca2+ channels and to a subtype of alpha 1-adrenoceptors.

CI 951 is a novel dihydronaphthyl Ca2+ antagonist and channel blocker.

AJG-049 free base is a calcium channel antagonist that inhibits L-type Ca2+ channels via diltiazem-binding site(s).

Cell-permeable calmodulin (CaM) antagonist that binds to the EF-hand/Ca2+-binding site. CALP2 has been demonstrated to inhibit CaM-dependant phosphodiesterase activity and increase intracellular Ca2+ concentrations by modulating Ca2+-channel activity. CAL

Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a long-acting, non-selective calcium channel (Ca+ channel) antagonist, an inhibitor of the Na+, K+ channel, and an inhibitor of cardiac Na+ Ca2+ exchange (NCX1).

AJG-049 HCl is a calcium channel antagonist that inhibits L-type Ca2+ channels via diltiazem-binding site(s).

SM-6586 is a potent calcium channel antagonist with inhibitory effects on Na+ H+ and Na+ Ca2+ exchange channels, and can be used in the study of cerebrovascular disease and hypertension, among other diseases.

(R)-(-)-Niguldipine hydrochloride is a L-type Ca2+ channel blocker and α1A-adrenoceptor antagonist.

TTA-Q6 (isomer) is an isomer of TTA-Q6, which functions as a selective antagonist of the T-type Ca2+ channel.