Na+/Ca2+ Exchanger Inhibitor

CGP37157 is a potent, selective inhibitor of Na⁺/Ca²⁺ exchanger, inhibiting the Na⁺-induced Ca²⁺-release from guinea-pig heart mitochondria, with an IC₅₀ of 0.8 μM.

SEA0400 is a novel and selective inhibitor of the Na⁺-Ca²⁺ exchanger (NCX), inhibiting Na⁺-dependent Ca²⁺ uptake in cultured neurons, astrocytes, and microglia with IC₅₀s of from 5 to 33 nM.

PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC₅₀s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC₅₀~0.9 mM) and recombinant P2Y4 (IC₅₀~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca²⁺ exchanger in guinea pig airway smooth muscle.

Parethoxycaine (Intracaine) is an ester-type local anesthetic that possesses dual activities as a non-selective inhibitor and agonist potentiator in smooth muscle, while acting as a mixed-type inhibitor of cytochrome c oxidase at the enzyme level. Parethoxycaine non-competitively inhibits the contraction of guinea pig ileal longitudinal muscle by interfering with transmembrane Ca²⁺ transport (blocking K⁺/CD responses in an equi-effective manner), and potentiates norepinephrine (NA) responses in rat vas deferens by blocking NA uptake and promoting Ca²⁺ mobilization (increasing the maximum amplitude without affecting K⁺ responses). Parethoxycaine inhibits the activity of purified cytochrome c oxidase in a concentration-dependent manner, and can be used in research focusing on Ca²⁺ signal transduction, smooth muscle contraction regulation, and mitochondrial energy metabolism.

Dichlorobenzamil (3',4'-Dichlorobenzamil; L-594881) hydrochloride is a Na⁺-Ca²⁺ Exchanger inhibitor. Dichlorobenzamil (hydrochloride) attenuates the Na⁺-Ca²⁺ exchanger-mediated inward current induced by activation of type I metabotropic glutamate receptors in second-order baroreceptor neurons of the rat nucleus tractus solitarius.

SAR296968 is a Na⁺/Ca²⁺ exchanger (NCX) subtype inhibitor with an IC₅₀ value of 74 nM against hNCX1. SAR296968 inhibits both forward and reverse modes of NCX current. SAR296968 enhances cardiac contractility and stroke volume. SAR296968 exerts antiarrhythmic effects. SAR296968 is applicable to research related to heart failure.

Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na⁺/Ca²⁺ exchanger (NCX) inhibitor (IC₅₀~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca²⁺-activated currents, with an IC₅₀ of 1.1 μM.

KB-R7943 mesylate is a widely used inhibitor of the reverse Na⁺/Ca²⁺ exchanger (NCX_rev) with IC₅₀ of 5.7±2.1 μM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.

SN 6 is a selective Na⁺/Ca²⁺ exchanger (NCX) inhibitor, and inhibits ⁴⁵Ca²⁺ uptake by NCX1, NCX2, and NCX3, with IC₅₀s of 2.9, 16, and 8.6 μM, respectively.

ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC₅₀ values of 67 and 55 nM for the reverse and forward mode inhibition, respectively. ORM-10962 shows antiarrhythmic effect.

ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger (NCX), which decreases the NCX current with estimated IC₅₀s of 55 and 67 nM at -80 and at 20 mV, respectively.

YM-244769 is a potent, selective and orally active Na⁺/Ca²⁺ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca²⁺ entry mode), with IC₅₀s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice.

YM-244769 dihydrochloride is a potent, selective and orally active Na⁺/Ca²⁺ exchanger (NCX) inhibitor. YM-244769 dihydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca²⁺ entry mode), with IC₅₀s of 18 nM and 50 nM, respectively. YM-244769 dihydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 dihydrochloride can also increase urine volume and urinary excretion of electrolytes in mice.

SEA0400 (Standard) is the analytical standard of SEA0400. This product is intended for research and analytical applications. SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger (NCX), inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.

YM-244769 hydrochloride is a potent, selective and orally active Na⁺/Ca²⁺ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca²⁺ entry mode), with IC₅₀s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice.

Caldaret is an intracellular Ca²⁺ handling modulator that acts through reverse mode Na⁺/Ca²⁺ exchanger inhibition.

Na⁺-Ca²⁺ Exchanger inhibitory peptide (XIP) is a Na⁺-Ca²⁺ exchanger inhibitor with a K_i of 200 nM. Na⁺-Ca²⁺ Exchanger inhibitory peptide inhibits the Na⁺-dependent Ca²⁺ uptake and the Na⁺-dependent Ca²⁺ efflux of sarcolemmal vesicles in a noncompetitive manner.

KB-R7943 (compound 1) is an inhibitor of sodium-calcium exchanger with an IC₅₀ value of 5.1 μM. KB-R7943 can be used as a tool in heart and renal failure models.

Benzamil (Benzylamiloride), an Amiloride analogue, is a Na⁺/Ca²⁺ exchanger (NCX) inhibitor (IC₅₀~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca²⁺-activated currents, with an IC₅₀ of 1.1 μM.

Dichlorobenzamil (3',4'-Dichlorobenzamil; L-594881) is an effective Na/Ca exchange inhibitor. Dichlorobenzamil significantly inhibits ⁴⁵Ca uptake mediated by reverse Na/Ca exchange in pancreatic islet cells (IC₅₀ = 18 μM). Dichlorobenzamil can also block K⁺ channels and voltage-sensitive Ca²⁺ channels.