1. GPCR/G Protein Neuronal Signaling
  2. Neurokinin Receptor
  3. L-733060 hydrochloride

L-733060 hydrochloride 

目录号: HY-14406A 纯度: ≥99.0%
COA 产品使用指南

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。

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L-733060 hydrochloride Chemical Structure

L-733060 hydrochloride Chemical Structure

CAS No. : 148687-76-7

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2].

IC50 & Target[1]

NK1

 

体外研究
(In Vitro)

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[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].

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

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.
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 μg/kg in conscious or anaesthetised rats[1].

MCE 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[1]
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.
分子量

439.82

Formula

C20H20ClF6NO

CAS 号
性状

固体

颜色

White to off-white

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 中的溶解度 : 22 mg/mL (50.02 mM; 加热助溶)

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
查看完整储备液配制表

* 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

L-733060 hydrochloride 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.2737 mL 11.3683 mL 22.7366 mL 56.8414 mL
5 mM 0.4547 mL 2.2737 mL 4.5473 mL 11.3683 mL
10 mM 0.2274 mL 1.1368 mL 2.2737 mL 5.6841 mL
15 mM 0.1516 mL 0.7579 mL 1.5158 mL 3.7894 mL
20 mM 0.1137 mL 0.5684 mL 1.1368 mL 2.8421 mL
25 mM 0.0909 mL 0.4547 mL 0.9095 mL 2.2737 mL
30 mM 0.0758 mL 0.3789 mL 0.7579 mL 1.8947 mL
40 mM 0.0568 mL 0.2842 mL 0.5684 mL 1.4210 mL
50 mM 0.0455 mL 0.2274 mL 0.4547 mL 1.1368 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
L-733060 hydrochloride
目录号:
HY-14406A
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