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

L-733060 是一种选择性的神经激肽-1 受体 (NK-1 receptor) 拮抗剂。L-733060 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 阻断 Substance P 在海马体中对长时程增强 (LTP) 的促进作用。L-733060 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 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 可用于研究慢性口面部疼痛和恶性黑色素瘤。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

L-733060

L-733060 Chemical Structure

CAS No. : 148700-85-0

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

L-733060 的其他形式现货产品:

Customer Review

Other Forms of L-733060:

L-733060 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Neurokinin Receptor 亚型特异性产品:

查看所有亚型
NK1R NK2R NK3R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 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 can be used for the study of chronic orofacial pain[1][2][3].

IC50 & Target[1][2]

NK1R

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
0.87 nM
Compound: 1
Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells
Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells
10.1016/0960-894X(95)00009-I
CHO IC50
0.87 nM
Compound: 4
Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells
Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells
[PMID: 8627597]
CHO IC50
1 nM
Compound: (+/-)2 (2S, 3S)
Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells
Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells
10.1016/S0960-894X(01)80280-8
CHO IC50
1 nM
Compound: 2
Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells
Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells
10.1016/0960-894X(95)00220-N
CHO IC50
1 nM
Compound: 2
Ability to displace [125I]-substance P from hNK1 receptor in chinese hamster ovarian (CHO) cells
Ability to displace [125I]-substance P from hNK1 receptor in chinese hamster ovarian (CHO) cells
[PMID: 9873445]
CHO IC50
1 nM
Compound: 4
Binding affinity at human tachykinin receptor 1 by measuring its ability to displace [125I]-labeled substance P from the cloned receptor expressed in CHO cells.
Binding affinity at human tachykinin receptor 1 by measuring its ability to displace [125I]-labeled substance P from the cloned receptor expressed in CHO cells.
[PMID: 9804702]
CHO IC50
1 nM
Compound: L-733060
Binding affinity for human NK1 receptor expressed in CHO cells
Binding affinity for human NK1 receptor expressed in CHO cells
10.1016/S0960-894X(01)80585-0
分子量

403.36

Formula

C20H19F6NO
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

L-733060 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

L-733060148700-85-0L733060L 733060Neurokinin ReceptorNK receptorTachykinin receptorNK-1 receptor antagonistorofacial hyperalgesiarostral ventromedial medulladescending pain modulationchronic pain maintenanceInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
L-733060
目录号：
HY-14406
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z