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-sensitivepotassium channel(KATP) opener, as well as an α4β2-containingnicotinic acetylcholine receptor (nAChR)antagonist[1]. |
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[1].
Iptakalim has an inhibitory effect on [Ca2+]cyt increase and the proliferation of pulmonary arterial SMCs induced by endothelin-1 through activation of KATPchannels. Iptakalim (10 μM, 10 min) pretreatment of pulmonary arterial SMCs significantly prevents ransient ncrease of [Ca2+]cyt elicited by endothelin-1[2].
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[2].
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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[3].
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Iptakalim (60 mg/kg) pretreatment significantly reduced activity (LSD comparisons)[3].
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| Animal Model: | Thirty male Sprague-Dawley rats weighing 275-299 grams[3]. | | 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).
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 25 mg/mL(139.10 mM;ultrasonic and warming and heat to 70℃) 配制储备液 | 1 mM | 5.5639 mL | 27.8195 mL | 55.6390 mL | | 5 mM | 1.1128 mL | 5.5639 mL | 11.1278 mL | | 10 mM | 0.5564 mL | 2.7820 mL | 5.5639 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 100 mg/mL (556.39 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
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