The sodium-hydrogen exchanger isoform-1 (NHE-1) is the predominant isoform of the Na+/H+ exchanger and is expressed in the heart where it contributes to cardiomyocyte pH homeostasis.{22706} It plays an important role in the myocardial response to ischemia-reperfusion.{22816} Cariporide is a benzoylguanidine compound that inhibits NHE-1 with IC50 values ranging from 0.03-3.4 µM.{22706} It displays selectivity for NHE-1 over NHE-2, NHE-3, and NHE-5 (IC50s = 4.3-62, 1->100, and >30 µM, respectively).{22706} The cardioprotective efficacy of cariporide has been examined in clinical investigations of patients at risk for myocardial infarction.{22706,22816}
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A benzoylguanidine compound that selectively inhibits NHE-1 (IC50s range from 0.03-3.4 µM)
Formal name: N-(aminoiminomethyl)-4-(1-methylethyl)-3-(methylsulfonyl)-benzamide
Synonyms: HOE 642
Molecular weight: 283.3
CAS: 159138-80-4
Purity: ≥95%
Formulation: A crystalline solid
Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction
The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}
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