L-733060 hydrochloride|cas:148687-76-7|西域试剂

L-733060 hydrochloride,99.0%

产品编号：Bellancom-14406A| CAS NO：148687-76-7| 分子式：C₂₀H₂₀ClF₆NO| 分子量：439.82

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-14406A		￥2600.00	杭州北京（现货）

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L-733060 hydrochloride

产品介绍

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 tachykinin NK₁ receptor antagonist. 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.

体外研究

L-733060 (30-300 nM) inhibits the [Ca²⁺]_i mobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK₁ receptor-transfected CHO cells.
L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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.

体内研究
(In Vivo)

L-733060 (10-1000 μg/kg; i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats.
L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000 μg/kg in conscious or anaesthetised rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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。

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)

参考文献