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- 2025年12月05日
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-20°C, sealed storage, away from moisture
- 库存：
货期：1-2天
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MedChemExpress LLC
- CAS号：
2387505-59-9
- 规格：
5 mg
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AP14145 hydrochloride
CAS No. : 2387505-59-9
MCE 国际站：AP14145 hydrochloride
产品活性：AP14145 hydrochloride 是一种有效的 KCa2 (SK) 通道负变构调节剂，对 KCa2.2 (SK2) 和 KCa2.3 (SK3) 通道的 IC50 均为 1.1 μM。AP14145 hydrochloride 的抑制作用很大程度上取决于通道中的两个氨基酸 S508 和 A533。AP14145 hydrochloride 延长了大鼠的心房有效不应期 (AERP)，并在耐 Vernakalant 的房颤 (AF) 猪模型中显示了抗心律失常作用。
研究领域：Membrane Transporter/Ion Channel
作用靶点：Potassium Channel
In Vitro: 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.
In Vivo: 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 t½ of 24.3 minutes in landrace pigs (12-13 weeks old, 30-35 kg gilts).
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文献和实验, laboratory-adapted HIV-1 (HXB2) can be divided into modulatory, core promoter, and transactivating regions (Fig. 1 ). The modulatory regions include elements with limited homology to AP-1 enhancer sequences at positions −347 to −329 relative to the cap site
Rapid Inactivation of Proteins by Knocksideways
, the small molecule, the cell or organism, and the assay. Curr. Protoc. Cell Biol . 61:15.20.1?15.20.7. © 2013 by John Wiley & Sons, Inc. Keywords: clathrin; AP?1; AP?2; rapamycin; AP21967
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