产品
编 号：F715407
分子式：C18H18ClF3N4O
分子量：398.81
分子式：C18H18ClF3N4O
分子量：398.81
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CAS No: 2387505-59-9
产品详情
生物活性：
AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
体内研究：
AP14145 (10 μM) increases the duration of the atrial effective refractory period (AERP) in isolated perfused rat hearts. AP14145 (2.5 and 5 mg/kg; bolus injections (iv)) increases the duration of the atrial effective refractory period in male sprague-dawley rats (250-350 g, 1-3 months old). AP14145 (5 mg/kg; bolus injections) has a Cmax of 8355 nmol/L, a t? of 24.3 minutes in landrace pigs (12-13 weeks old, 30-35 kg gilts).
体外研究：
AP14145 (10 nM-30 μM) inhibits both hKCa2.2 and hKCa2.3 channel currents in a concentration‐dependent fashion. AP14145 (10 μM) inhibits 50% of the hKCa1.1 current, 90% of the hKCa2.1 current and has no effect on hKCa3.1 channel. AP14145 (10 μM) increases the EC50 of Ca2+ on KCa2.3 channels from 0.36 to 1.2 μM. AP14145 hydrochloride demonstrates an IC50 in whole-cell patch clamp on the human SK3 channel of 1.3 μM. AP14145 inhibits hERG (KV11.1) with an IC50 of 71.8 μM and Kir3.1/Kir3.4 (IKACh) with an IC50 of 9.3 μM and does not produce any significant effects on KV1.5 (IKur), KV7.1/KCNE1 (IKs), KV4.3/KChiP2 (Ito), and Kir2.1 (IK1) in 30 μM or on NaV1.5 (15 μM; INa) on a panel of cardiac ion channels. AP14145 (1-10 μM) produces no significant block of CaV1.2.
AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
体内研究：
AP14145 (10 μM) increases the duration of the atrial effective refractory period (AERP) in isolated perfused rat hearts. AP14145 (2.5 and 5 mg/kg; bolus injections (iv)) increases the duration of the atrial effective refractory period in male sprague-dawley rats (250-350 g, 1-3 months old). AP14145 (5 mg/kg; bolus injections) has a Cmax of 8355 nmol/L, a t? of 24.3 minutes in landrace pigs (12-13 weeks old, 30-35 kg gilts).
体外研究：
AP14145 (10 nM-30 μM) inhibits both hKCa2.2 and hKCa2.3 channel currents in a concentration‐dependent fashion. AP14145 (10 μM) inhibits 50% of the hKCa1.1 current, 90% of the hKCa2.1 current and has no effect on hKCa3.1 channel. AP14145 (10 μM) increases the EC50 of Ca2+ on KCa2.3 channels from 0.36 to 1.2 μM. AP14145 hydrochloride demonstrates an IC50 in whole-cell patch clamp on the human SK3 channel of 1.3 μM. AP14145 inhibits hERG (KV11.1) with an IC50 of 71.8 μM and Kir3.1/Kir3.4 (IKACh) with an IC50 of 9.3 μM and does not produce any significant effects on KV1.5 (IKur), KV7.1/KCNE1 (IKs), KV4.3/KChiP2 (Ito), and Kir2.1 (IK1) in 30 μM or on NaV1.5 (15 μM; INa) on a panel of cardiac ion channels. AP14145 (1-10 μM) produces no significant block of CaV1.2.
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