2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. FMJ-01-054

FMJ-01-054 是一种选择性多巴胺 D4 受体 (D4R) 拮抗剂，其 Ki 值为 77.7 nM。FMJ-01-054 对 D2R 和 D3R 具有亚型选择性。FMJ-01-054 能抑制 D4R 介导的 β--arrestin 招募和 cAMP 生成，其 IC50 值分别为 3800 nM 和 134 nM。FMJ-01-054 在大鼠体内具有理想的血浆半衰期和脑部暴露量。FMJ-01-054 可用于神经精神疾病研究。

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

FMJ-01-054

FMJ-01-054 Chemical Structure

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.

Customer Review

FMJ-01-054 相关抗体

Top Publications Citing Use of Products

查看 Dopamine Receptor 亚型特异性产品:

查看所有亚型
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FMJ-01-054 is a selective dopamine D4 Receptor (D4R) antagonist with a Ki od 77.7 nM. FMJ-01-054 shows subtype selectivity over D2R and D3R. FMJ-01-054 inhibits D4R-mediated β-arrestin recruitment and cAMP production with IC50 values of 3800 nM and 134 nM, respectively. FMJ-01-054 has desirable plasma half-life and brain exposure in rats. FMJ-01-054 can be used for the research of neurological disorders[1].

IC50 & Target

Human D4 Receptor

77.7 nM (Ki)

Human D2 Receptor

>100,000 nM (Ki)

Human D3 Receptor

>100,000 nM (Ki)

体外研究
(In Vitro)

FMJ-01-054 (compound 17) (0.3 nM-100 μM；1 h) 以高亲和力与人多巴胺 D4 受体结合 (Ki = 77.7 nM)，且对 D2 和 D3 受体的选择性大于 1287 倍[1]。
FMJ-01-054 是人多巴胺 D4 受体的拮抗剂，其 IC50 为 3800 nM，且无激动剂活性[1]。
FMJ-01-054 (30 min) 作为拮抗剂可抑制多巴胺 D4 受体介导的 cAMP 生成，其 IC50 为 134 nM[1]。
FMJ-01-054 在大鼠和人肝微粒体中表现出代谢稳定性，半衰期分别为 64.77 min 和 46.84 min[1]。

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

FMJ-01-054 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat[1] 5 mg/kg i.p. Tmax 0.25 h
Rat[1] 5 mg/kg i.p. Brain-to-Plasma Ratio 0.3
体内研究
(In Vivo)

FMJ-01-054 (compound 17) (5 mg/kg；腹腔注射；单剂量) 在 Sprague−Dawley 大鼠中表现出良好的体内药代动力学特性 (血浆半衰期为 2.10 小时，脑 Cmax 为 3.04 nmol/g，脑血比为 0.30)[1]。

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

368.86

Formula

C19H21ClN6
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

FMJ-01-054 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:

FMJ-01-054Dopamine Receptorratssubstance use disordersD3Ramide analogshuman dopamine D? receptorblood-brain barrierD4RschizophreniaSprague?Dawley ratsl-dopa-induced dyskinesiasDopamine D4 ReceptorD2Rattention-deficit/hyperactivity disordercAMPβ-arrestin recruitmenthuman liver microsomesrat liver microsomesInhibitorinhibitorinhibit

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：
FMJ-01-054
目录号：
HY-181049
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