Cariporide

SKU: orb1226078

Description

Cariporide (HOE642)is a potent, selective sodium-hydrogen exchange subtype 1 (NHE1) inhibitor with IC50 of 50 nM, little to no activity against NHE3 and NHE2 (IC50=3 and 10 uM); inhibits the amiloride sensitive sodium influx in rabbit erythrocytes, reduces the swelling of human platelets induced by intracellular acidification, and delays pH recovery in rat cardiomyocytes; reduces and prevents ventricular premature beats, ventricular tachycardia, and ventricular fibrillation after oral treatment in vivo, shows cardioprotective and antiarrhythmic effects in ischaemic and reperfused hearts.Heart Arrhythmia Phase 2 Discontinued(In Vitro):Cariporide significantly suppresses markers of cell death, such as TUNEL positivity and caspase-3 cleavage, at 8 or 16 hours. Cariporide remarkably suppresses cytosolic Na+ and Ca2+ accumulation. Cariporide prevents mitochondrial membrane potential loss induced by H2+O2+. Cariporide (HOE-642) ameliorates myocardial ischemia/reperfusion injury, by the well-established reduction of cytosolic Ca2+ in cardiac myocytes through inhibition of Na+/H+ exchange. Cariporide (HOE-642), has inhibitory effects on the degranulation of human platelets, the formation of platelet–leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1).(In Vivo):Intravenous administration of cariporide significantly decreases brain Na+ uptake and reduces cerebral edema, brain swelling, and infarct volume.

Key Properties

• CAS Number: 159138-80-4
• MW: 283.346
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₇N₃O₃S
• SMILES: O=C(/N=C(N)\N)C1=CC=C(C(C)C)C(S(=O)(C)=O)=C1
• Target: Sodium Channel
• Solubility: DMSO: 79 mg/mL (278.8 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Intravenous administration of cariporide significantly decreases brain Na+ uptake and reduces cerebral edema, brain swelling, and infarct volume.
• In Vitro:
  Cariporide significantly suppresses markers of cell death, such as TUNEL positivity and caspase-3 cleavage, at 8 or 16 hours. Cariporide remarkably suppresses cytosolic Na+ and Ca2+ accumulation. Cariporide prevents mitochondrial membrane potential loss induced by H2+O2+. Cariporide (HOE-642) ameliorates myocardial ischemia/reperfusion injury, by the well-established reduction of cytosolic Ca2+ in cardiac myocytes through inhibition of Na+/H+ exchange. Cariporide (HOE-642), has inhibitory effects on the degranulation of human platelets, the formation of platelet-leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HOE642 | HOE-642

Quick Database Links

Gene Symbol

Sodium Channel