AP14145 hydrochloride T39963
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
5 mg | 2387505-59-9 | ¥5,400.00 | 询底价 |
Product Introduction
Bioactivity
英文名: AP14145 hydrochloride
描述: AP14145 hydrochloride is a potent negative allosteric modulator of K Ca 2 (SK) channels, specifically targeting K Ca 2.2 (SK2) and K Ca 2.3 (SK3) channels with an IC 50 of 1.1 μM. Inhibition of AP14145 hydrochloride is highly influenced by S508 and A533 amino acids present in the channel. This compound effectively extends the atrial effective refractory period (AERP) in rats and exhibits antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
体外活性: AP14145 (10 nM-30 μM) inhibits both hK Ca 2.2 and hK Ca 2.3 channel currents in a concentration‐dependent fashion. AP14145 (10 μM) inhibits 50% of the hK Ca 1.1 current, 90% of the hK Ca 2.1 current and has no effect on hK Ca 3.1 channel. AP14145 (10 μM) increases the EC 50 of Ca 2+ on K Ca 2.3 channels from 0.36 to 1.2 μM[1]. AP14145 hydrochloride demonstrates an IC 50 in whole-cell patch clamp on the human SK3 channel of 1.3 μM. AP14145 inhibits hERG (K V 11.1) with an IC 50 of 71.8 μM and K ir 3.1/K ir 3.4 (I KACh ) with an IC 50 of 9.3 μM and does not produce any significant effects on K V 1.5 (I Kur ), K V 7.1/KCNE1 (I Ks ), K V 4.3/KChiP2 (I to ), and K ir 2.1 (I K1 ) in 30 μM or on Na V 1.5 (15 μM; I Na ) on a panel of cardiac ion channels. AP14145 (1-10 μM) produces no significant block of Ca V 1.2[2].
体内活性: AP14145 (10 μM) increases the duration of the atrial effective refractory period (AERP) in isolated perfused rat hearts[1]. 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)[1]. AP14145 (5 mg/kg; bolus injections) has a C max of 8355 nmol/L, a t ? of 24.3 minutes in landrace pigs (12-13 weeks old, 30-35 kg gilts)[2].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字: AP14145 hydrochloride | AP-14145 hydrochloride | AP-14145 Hydrochloride | AP 14145 Hydrochloride | AP14145 Hydrochloride
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