Iptakalim Hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Iptakalim 是一种亲脂性对氨基化合物，是一种新型 ATP 敏感钾通道 (KATP) 开放剂，也是一种含有 α4β2 的烟碱乙酰胆碱受体 (nAChR) 拮抗剂。

Iptakalim, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist. Iptakalim is also a K(ir) 6.1/SUR2B activator that can attenuate hypoxia-induced pulmonary arterial hypertension in rats by endothelial function protection.

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 [Ca2+]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 [Ca2+]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.

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).. Animal Model:Thirty male Sprague-Dawley rats weighing 275-299 grams.Dosage:0, 10, 30, or 60 mg/kg.Administration:IP, 10 min before the start of a 4-min test session.Result:Decreased chamber activity.Dipper entries following pretreatment with 30 and 60 mg/kg Iptakalim were significantly lower than with 0 (saline) or 10 mg/kg iptakalim pretreatment (Tukey HSD tests).

——

Cell Cycle/DNA Damage

Potassium Channel

Aldose reductase

——

——

642407-63-4

179.73

C9H22ClN

>98% (HPLC)

In Vitro:?H2O : 25 mg/mL (139.10 mM)

Cl.CC(C)NC(C)(C)C(C)C

——

(-20℃)

With Ice Pack

≥ 2 years