1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. RWJ-51204

RWJ-51204 是 GABA(A) receptor 的部分激动剂,Ki 值为 0.2-2 nM。

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

RWJ-51204 Chemical Structure

RWJ-51204 Chemical Structure

CAS No. : 205701-85-5

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 价格 是否有货
1 mg ¥3995
询问价格 & 货期

* Please select Quantity before adding items.

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

IC50 & Target

Ki: 0.2-2 nM (GABA(A))[1]

体外研究
(In Vitro)

RWJ-51204 binds to receptors in the cerebral cortex, cerebellum, or medulla-spinal cord with Ki ranging from 0.2 to 0.6 nM.

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

体内研究
(In Vivo)

RWJ-51204 is orally active in anxiolytic efficacy tests. WJ 51204 dose-relatedly antagonizes PTZ-induced clonic convulsions when administered orally (ED50 = 0.04 mg/kg). RWJ-51204 is effective in the conflict test in monkeys (ED50 of approximately 0.5 mg/kg p.o.). RWJ-51204 potently impairs rotarod performance in rats (ED50 = 0.12 mg/kg), and all rats given RWJ-51204 orally at 30 mg/kg exhibit sedation, reduced skeletal muscle tone, and impairment of rotarod performance.

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

分子量

399.39

Formula

C21H19F2N3O3

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
Kinase Assay
[1]

For each sample, a portion of the membrane fraction containing 0.1 to 0.2 mg of protein is incubated in 2 mL of a 3 mM phosphate-buffered solution containing 0.1 M NaCl and 0.01 to 0.03 μCi of a 3H-labeled ligand [3H]Ro15-4513, [3H]flumazenil. The receptor-ligand binding reaction is allowed to reach equilibrium at an ambient temperature of 21-23°C (30 min) and then the reaction is terminated by vacuum filtration to separate the incubation medium from the biological membranes. The membrane samples are washed to remove unbound ligand. The3H bound to each membrane sample is quantified using liquid scintillation spectrometry.

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

Animal Administration
[1]

Adult rats are deprived of water for 48 h and are deprived of food for at least 16 h before testing. After the first 24 h of water deprivation, they are placed in a sound-attenuating chamber for a training period, in which they are allowed 200 licks from a bottle containing tap water. The experiment is performed the next day. Vehicle or compounds are administered orally by gavage, and at specified times after dosing, rats are placed in the chamber and allowed access to tap water. The first lick at the stainless steel sipper tube of a water bottle initiates a 3-min test session in which every 20th lick is punished by a 0.2 s, 0.5 mA shock (root mean square, measured across the electrodes) delivered via the sipper tube. If rats fail to drink within 5 min, the experiment is terminated, and they are evaluated for signs of CNS depression. Rats are not reused in this experiment. The anxiolytic effectiveness of a compound in this assay is determined from the number of rats, at each dose, that receive a number of shocks that is equal to or greater than the calculated 90th percentile of the number of shocks received by approximately 600 vehicle-treated rats. This criterion is eight shocks when rats are tested 1 h after administration and 10 shocks when rats are tested 4 h after administration.

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

参考文献
  • 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.

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:
RWJ-51204
目录号:
HY-19308
需求量: