4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Iptakalim hydrochloride 是亲脂性的对氨基化合物,是 ATP 敏感的钾通道 (KATP) 的开放剂,也是包含α4β2 的烟碱乙酰胆碱受体 (nAChR)拮抗剂。
生物活性
Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (K ATP ) opener, as well as an α 4 β 2 -containing nicotinic acetylcholine receptor (nAChR) antagonist.
性状
Solid
体外研究(In Vitro)
Iptakalim (Ipt) hydrochloride has been shown to reverse pulmonary resistance vascular remodeling, inhibit proliferation of pulmonary arterial smooth muscle cells (PASMCs) and airway smooth muscle cells (ASMCs), as well as protect PAECs from pathological stimulation.Iptakalim has an inhibitory effect on [Ca]cyt increase and the proliferation of pulmonary arterial SMCs induced by endothelin-1 through activation of KATP channels. Iptakalim (10 μM, 10 min) pretreatment of pulmonary arterial SMCs significantly prevents ransient ncrease of [Ca]cyt elicited by endothelin-1.Iptakalim at he concentrations of 0.1, 1, and 10 AM lowered[3H]thymidine incorporation by 19.75±4.60% (n=10), 41.20±9.49% (n=10), and 54.74±10.11% (n=10), respectively, compared with that of cells treated only with endothelin-1.
体内研究(In Vivo)
Iptakalim (10-60 mg/kg) attenuates nicotine-evoked conditioned responding. Iptakalim also attenuates chamber activity in these nicotine test sessions..
Iptakalim (60 mg/kg) pretreatment significantly reduced activity (LSD comparisons).. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Mengyu He, et al. Iptakalim ameliorates hypoxia-impaired human endothelial colony-forming cells proliferation, migration, and angiogenesis via Akt/eNOS pathways. Pulm Circ. 2019 Oct 18;9(3):2045894019875417.[2]. Weiping Xie, et al. Anti-proliferating effect of iptakalim, a novel KATP channel opener, in cultured rabbit pulmonary arterial smooth muscle cells. Eur J Pharmacol. 2005 Mar 28;511(2-3):81-7.
溶解度数据
In Vitro: H2O : 25 mg/mL (139.10 mM; ultrasonic and warming and heat to 70°C)配制储备液