L-733060 hydrochloride 是一种有效的速激肽NK1受体拮抗剂。 L-733060 hydrochloride 以不会在啮齿动物中引起不良心血管影响的剂量抑制神经源性血浆外渗，同时还充当抗肿瘤剂。
| 生物活性 | L-733060 hydrochloride is a potent tachykininNK1receptorantagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent[1][2]. |
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体外研究
(In Vitro) | L-733060 (30-300 nM) inhibits the [Ca2+]imobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK1receptor-transfected CHO cells[1].
L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells[2].
L-733060 (10-30 μM; 24 and 48 h) inhibits MEL H0 cells proliferation with IC50s of 27.5 μM and 18.9 μM at 24 h and 48 h, respectively[2].
L-733060 (20-50 μM; and or 72 h) inhibits COLO 679 cells growth with IC50s of 33.8 μM and 31.5 μM at 30 h and 72 h, respectively[2].
Cell Proliferation Assay[2] | Cell Line: | COLO 858 cells | | Concentration: | 2.5, 5, 10, 20 μM | | Incubation Time: | 0, 48, 96 h | | Result: | Inhibited cells growth with IC50s of 8.7 μM and 7.1 μM at 48 h and 96 h, respectively. |
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体内研究
(In Vivo) | L-733060 (10-1000 μg/kg; i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats[1].
L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of<3000 μgkg in conscious or anaesthetised rats[1].
| Animal Model: | Male Sprague-Dawley rats (200 g) with electrical stimulation of the trigeminal ganglion[1] | | Dosage: | 10, 100, 1000 mg/kg | | Administration: | I.v. injection | | Result: | Produced a significant dose-related inhibition of plasma extravasation with an ID50of 212±19 μg/kg. |
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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 : 22 mg/mL(50.02 mM;Need warming) 配制储备液 | 1 mM | 2.2737 mL | 11.3683 mL | 22.7366 mL | | 5 mM | 0.4547 mL | 2.2737 mL | 4.5473 mL | | 10 mM | 0.2274 mL | 1.1368 mL | 2.2737 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。 |
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