Ketanserin tartrate

• CAT Number: I005020
• CAS Number: 83846-83-7
• Molecular Formula: C22H22FN3O3 • C4H6O6
• Molecular Weight: 545.52
• Purity: ≥95%
• Target: 0.11 μM (hERG current)[1]
• Solubility: H2O: ≤ 30 mg/mL (Need ultrasonic and warming)
• Storage: 2-8°C
• IUPAC Name: 2,3-dihydroxybutanedioic acid;3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione
• InChI: InChI=1S/C22H22FN3O3.C4H6O6/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29;5-1(3(7)8)2(6)4(9)10/h1-8,16H,9-14H2,(H,24,29);1-2,5-6H,(H,7,8)(H,9,10)
• InChIKey: KMTLTEVOQLMYRS-UHFFFAOYSA-N
• SMILES: C1CN(CCC1C(=O)C2=CC=C(C=C2)F)CCN3C(=O)C4=CC=CC=C4NC3=O.C(C(C(=O)O)O)(C(=O)O)O

Ketanserin tartrate（Cat No.:I005020） is a selective antagonist of 5-HT receptors, which are involved in serotonin signaling. Additionally, it exhibits concentration-dependent blocking of hERG current (IhERG), with an IC50 value of 0.11 μM. This blocking effect on IhERG suggests a potential impact on cardiac repolarization, as hERG channels are involved in regulating the duration of action potentials in the heart.

Reference

[1]. Tang Q, et al. The 5-HT2 antagonist Ketanserin is an open channel blocker of human cardiac ether-à-go-go-related gene (hERG) potassium channels. Br J Pharmacol. 2008 Oct;155(3):365-73.
[2]. Khan N, et al. Investigation of cyclooxygenase and signaling pathways involved in human platelet aggregation mediated by synergistic interaction of various agonists. Drug Des Devel Ther. 2015 Jul 6;9:3497-506.
[3]. Kekewska A, et al. Antiserotonergic properties of terguride in blood vessels, platelets, and valvular interstitial cells. J Pharmacol Exp Ther. 2012 Feb;340(2):369-76.
[4]. Jiang DG, et al. Serotonin regulates brain-derived neurotrophic factor expression in select brain regions during acute psychological stress. Neural Regen Res. 2016 Sep;11(9):1471-1479.