Semotiadil recemate fumarate
Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel vasoselective Ca2+ channel antagonist.
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- CAS No.: 123388-25-0
- Formule: C33H36N2O10S
- Masse moléculaire:652.71
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
Ca2+ channel[1]
In Vitro
Semotiadil in a concentration of 1 μM produces an inhibition of 12.4±9.7% and in a concentration of 10 μM an inhibition of 25±11.0%[1]. Effects of Semotiadil on the voltage-dependent Ca current (ICa) are investigated in dispersed smooth muscle cells of the rabbit portal vein. At a holding potential of -100 mV, Semotiadil (> or =0.1 μM; dissolved in DMSO) inhibits the ICa in a concentration-dependent manner (IC50=2.0 μM). At a holding potential of -80 mV or -60 mV, the concentration-inhibition curve observed in the presence of Semotiadil is shifted to the left compared with that observed at -100 mV; and Semotiadil shifts the voltage-dependent inactivation curve to the left. The curve for the decay of ICa is fitted with two time constants. Semotiadil (<1 μM) reduces the slow but not the fast time constant. The curve for the recovery from ICa inactivation also consisted of two time constants, and Semotiadil (1 microM) prolongs the slow recovery. Semotiadil dissolved in deionized water more potently inhibits ICa than Semotiadil dissolved in DMSO[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 123388-25-0
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Masse moléculaire 652.71
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Formule C33H36N2O10S
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SMILES
O=C(O)/C=C/C(O)=O.O=C1C(C2=CC(OC)=CC=C2OCCCN(CCOC3=CC=C(OCO4)C4=C3)C)SC5=CC=CC=C5N1C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Koidl B, et al. A novel benzothiazine Ca2+ channel antagonist, Semotiadil, inhibits cardiac L-type Ca2+ currents. Eur J Pharmacol. 1997 Mar 19;322(2-3):243-7. [Content Brief]
[2]. Teramoto N. Mechanisms of the inhibitory action of Semotiadil fumarate, a novel Ca antagonist, on the voltage-dependent Ca current in smooth muscle cells of the rabbit portal vein. Jpn J Pharmacol. 1993 Mar;61(3):183-95. [Content Brief]
[3]. Ichikawa M, et al. Antihypertensive effects of a novel calcium antagonist, Semotiadil fumarate (SD-3211), alone and in combination with Enalapril or trichlormethiazide in spontaneously hypertensive rats. Biol Pharm Bull. 1994 Nov;17(11):1513-5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)