L-733,060 hydrochloride - CAS:148687-76-7

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L-733,060 hydrochloride

目录号 : KG12454 CAS No. : 148687-76-7 纯度 : 98%

Data Sheet SDS 产品使用指南

L-733060 hydrochloride 是一种选择性的神经激肽-1 受体 (NK-1 receptor) 拮抗剂。L-733060 hydrochloride 主要通过阻断 Substance P (P 物质) 与 NK-1 受体的结合来调控痛觉传递和神经可塑性能阻断 L-733060 hydrochloride 阻断 Substance P 在海马体中对长时程增强 (LTP) 的促进作用。L-733060 hydrochloride 逆转大鼠由实验性咬合干扰 (EOI) 诱导的口面部痛觉过敏。L-733060 hydrochloride 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。L-733060 hydrochloride 可用于研究慢性口面部疼痛和恶性黑色素瘤。

规格	价格	是否有货	数量
10mg		In-stock

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Other Forms of Rapamycin:

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L-733,060 hydrochloride In-stock

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生物活性

L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 hydrochloride mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 hydrochloride blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 hydrochloride reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 hydrochloride can be used for the study of chronic orofacial pain.

体外研究

L-733060 hydrochloride (30-300 nM) inhibited the [Ca2+]i mobilization induced by substance P (100 nM) in human neurokinin-1 receptor-transfected CHO cells in a concentration-dependent manner.
L-733060 hydrochloride (2.5-20 μM; 48 and/or 96 hours) induced concentration-dependent cytotoxicity in COLO 858 cells.
L-733060 hydrochloride (10-30 μM; 24 hours, 48 hours) inhibited the proliferation of MEL H0 cells at 24 hours and 48 hours, with IC50 values of 27.5 μM and 18.9 μM, respectively.
L-733060 hydrochloride (20-50 μM) inhibited the growth of COLO 679 cells at 30 hours and 72 hours, with IC50 values of 33.8 μM and 31.5 μM, respectively.

Cell Proliferation Assay

Cell Line:	COLO 858 cells
Concentration:	2.5, 5, 10, 20 μM
Incubation Time:	0, 48, 96 hours
Result:	Inhibited cells growth with IC₅₀s of 8.7 μM and 7.1 μM at 48 h and 96 h, respectively.

体内研究

L-733060 hydrochloride (10-1000 μg/kg; intravenous injection) inhibits electrically stimulated plasma extravasation in the dura mater of rats.
L-733060 hydrochloride (300-3000 μg/kg; intravenous injection) showed no significant hypotensive or bradycardic effects in conscious or anesthetized rats at doses below 3000 μg/kg.

Animal Model:	Male Sprague-Dawley rats (200 g) with electrical stimulation of the trigeminal ganglion
Dosage:	10, 100, 1000 mg/kg
Administration:	I.v. injection
Result:	Produced a significant dose-related inhibition of plasma extravasation with an ID₅₀ of 212±19 μg/kg.

分子式

C₂₀H₁₉F₆NO^.HCl

分子量

439.83

CAS号

148687-76-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°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

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

纯度： 98%