BRL-54443

价格	￥729.21
包装	1EA

最小起订量	1EA
发货地	其他
更新日期	2020-01-15

产品详情

英文名称:BRL-54443
规格: 10mg/10mM/1mL/50mg	货号: S2852

Selleck Chemicals美国品牌，中国库存现货，5-HT Receptor抑制剂，CAS#57477-39-1。
更多详情请访问中国唯一官方网站：
http://www.selleck.cn/products/brl-54443.html

生物活性

产品描述	BRL 54443是一种5-HT1E和5-HT1F受体激动剂，pK_i分别为8.7和9.25，对5-HT1A， 5-HT1B， 5-HT1D受体具有弱的结合亲和力。
靶点	5-HT_1E	5-HT_1F	5-HT_1A	5-HT_1B	5-HT_1D
IC50	8.7 (pK_i)	9.25 (pK_i)	7.2 (pK_i)	6.9 (pK_i)	7.2 (pK_i) ^[1]
体外研究	BRL 54443 has also measurable affinity for the 5-HT_2A receptor. BRL 54443 induces contraction with a −logEC50 of 6.52. Contraction caused by BRL 54443 is likely mediated through stimulation of 5-HT5-HT_2A receptors. ^[2]
体内研究	BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. ^[1]
临床实验
特征

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验: ^[1]

Membrane preparation and binding assay	The binding affinity of a set of 5-HT receptor agonists and antagonists (samples) at 5-HT_1F receptors is tested. To do this h5-HT_1F-HEK 293 cells are cultured in Petri dishes till 90% confluency is reached. The cells are scraped from the plates and suspended in 50 mM Tris–HCl buffer (pH 7.4). After centrifugation (23,500 × g) the pellet is suspended in 5 mM Tris–HCl buffer (pH 7.4) and homogenized with an Ultra Turrax homogeniser. The membranes are collected by centrifugation at 18,000 × g for 20 minutes, resuspended in 50 mM Tris–HCl (pH 7.4) and stored at −80 °C. At the day of the binding experiment, the membranes are defrosted and homogenized. The protein concentration is determined using the Bradford protein assay and the membranes are diluted in the assay buffer down to 65 μg protein/mL (50 mM Tris–HCl, 10 mM MgCl₂, 1 mM EGTA and 10 μM pargyline, pH 7.4). Assay mixtures (0.5 mL) contained 0.4 mL membrane preparation and 2 nM of tritiated 5-HT (118 Ci/mmol); to determine the non-specific binding 1 μM sumatriptan is added. Per sample studied 15 mixtures are created containing different concentrations (10 μM–1 pM) of the sample. The mixtures are then incubated for 60 minutes at 25 °C (protected from light), incubation is stopped by rapid filtration on a Filtermate 96. Bound radioactivity is determined by liquid scintillation counting. Data are analysed graphically with inhibition curves and IC50 values are derived. K_i values are calculated according to the equation K_i =IC50/(1+(C/K_d)), with C as the concentration of [³H]5-HT (2 nM) and K_d as the equilibrium dissociation constant of [³H]5-HT (2.61 nM).

Membrane preparation and binding assay

The binding affinity of a set of 5-HT receptor agonists and antagonists (samples) at 5-HT_1F receptors is tested. To do this h5-HT_1F-HEK 293 cells are cultured in Petri dishes till 90% confluency is reached. The cells are scraped from the plates and suspended in 50 mM Tris–HCl buffer (pH 7.4). After centrifugation (23,500 × g) the pellet is suspended in 5 mM Tris–HCl buffer (pH 7.4) and homogenized with an Ultra Turrax homogeniser. The membranes are collected by centrifugation at 18,000 × g for 20 minutes, resuspended in 50 mM Tris–HCl (pH 7.4) and stored at −80 °C. At the day of the binding experiment, the membranes are defrosted and homogenized. The protein concentration is determined using the Bradford protein assay and the membranes are diluted in the assay buffer down to 65 μg protein/mL (50 mM Tris–HCl, 10 mM MgCl₂, 1 mM EGTA and 10 μM pargyline, pH 7.4). Assay mixtures (0.5 mL) contained 0.4 mL membrane preparation and 2 nM of tritiated 5-HT (118 Ci/mmol); to determine the non-specific binding 1 μM sumatriptan is added. Per sample studied 15 mixtures are created containing different concentrations (10 μM–1 pM) of the sample. The mixtures are then incubated for 60 minutes at 25 °C (protected from light), incubation is stopped by rapid filtration on a Filtermate 96. Bound radioactivity is determined by liquid scintillation counting. Data are analysed graphically with inhibition curves and IC50 values are derived. K_i values are calculated according to the equation K_i =IC50/(1+(C/K_d)), with C as the concentration of [³H]5-HT (2 nM) and K_d as the equilibrium dissociation constant of [³H]5-HT (2.61 nM).

动物实验: ^[1]

动物模型	Adult male cats
配制	Distilled water containing 1 equivalent 2,3-dihydroxybutanedioic acid+0.9% NaCl
剂量	3 μg/kg-30 mg/kg
给药处理	s.c.

温馨提示：不可用于临床治疗。

关键字： BRL-54443;化学试剂

公司简介

成立日期		注册资本
员工人数		年营业额
主营行业		经营模式

Selleck中国

非会员

公司成立：暂无
注册资本：暂无
企业类型：暂无
主营产品：暂无
公司地址：

进入店铺

询盘

店内推荐

AMG-458

￥2186.15

6-Thio-dG

￥875.67

CP-91149

￥575.95

BRL-54443相关厂家报价

产品名称	价格		公司名称	报价日期
aladdin 阿拉丁 B129734 BRL-54443,5-HT 1E和5-HT 1F受体激动剂 57477-39-1 ≥98%	￥35.90	VIP12年	上海阿拉丁生化科技股份有限公司	2024-04-25
aladdin 阿拉丁 B409219 BRL-54443 57477-39-1 10mM in DMSO	￥957.90	VIP1年	上海阿拉丁生化科技股份有限公司	2024-04-22
BRL-54443	￥890		上海晶抗生物工程有限公司	2024-04-11
BRL-54443	￥729.21		上海超研生物科技有限公司	2024-04-11
BRL-54443	￥756		上海意杰生物科技有限公司	2024-04-11
BRL-54443	询价		上海禾午生物科技有限公司	2020-11-03
BRL-54443	￥370		上海嵘崴达实业有限公司	2020-01-16
BRL-54443	￥1885		上海经科化学科技有限公司	2020-01-16
BRL54443	询价		厦门研科生物技术有限公司	2020-01-14
BRL-54443	询价		上海熹垣生物科技有限公司	2020-01-14

内容声明:
以上所展示的信息由商家自行提供，内容的真实性、准确性和合法性由发布商家负责。商家发布价格指该商品的参考价格，并非原价，该价格可能随着市场变化，或是由于您购买数量不同或所选规格不同而发生变化。最终成交价格，请咨询商家，以实际成交价格为准。请意识到互联网交易中的风险是客观存在的