BRL-54443

價格	￥729.21
包裝	1EA

最小起訂量	1EA
發(fā)貨地	其他
更新日期	2020-01-15

產(chǎn)品詳情

英文名稱:BRL-54443
規(guī)格: 10mg/10mM/1mL/50mg	貨號: S2852

Selleck Chemicals美國品牌，中國庫存現(xiàn)貨，5-HT Receptor抑制劑，CAS#57477-39-1。
更多詳情請訪問中國唯一官方網(wǎng)站：
http://www.selleck.cn/products/brl-54443.html

生物活性

產(chǎn)品描述	BRL 54443是一種5-HT1E和5-HT1F受體激動劑，pK_i分別為8.7和9.25，對5-HT1A， 5-HT1B， 5-HT1D受體具有弱的結(jié)合親和力。
靶點	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]	?
體外研究	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]
體內(nèi)研究	BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. ^[1]
臨床實驗	?
特征	?

推薦的實驗操作(此推薦來自于公開的文獻所以Selleck并不保證其有效性)

激酶實驗: ^[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).

動物實驗: ^[1]

動物模型	Adult male cats
配制	Distilled water containing 1 equivalent 2,3-dihydroxybutanedioic acid+0.9% NaCl
劑量	3 μg/kg-30 mg/kg
給藥處理	s.c.?

溫馨提示：不可用于臨床治療。

關(guān)鍵字： BRL-54443;化學(xué)試劑

公司簡介

成立日期		注冊資本
員工人數(shù)		年營業(yè)額
主營行業(yè)		經(jīng)營模式

Selleck中國

普通會員

公司成立：暫無
注冊資本：暫無
企業(yè)類型：暫無
主營產(chǎn)品：暫無
公司地址：

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BRL-54443相關(guān)廠家報價

產(chǎn)品名稱	價格		公司名稱	報價日期
3-(1-甲基哌啶-4-基)-1H-吲哚-5-醇 57477-39-1	詢價	VIP5年	河南威梯?；た萍加邢薰?/div>	2025-06-18
BRL-54443	￥720		武漢科昊佳生物科技有限公司	2025-06-16
BRL-54443	￥2300		蘇州瑞諾德生物科技有限公司	2025-06-16
BRL54443	￥323		上海恪敏生物科技有限公司	2025-06-16
BRL-54443	￥85		上海彩佑實業(yè)有限公司	2025-06-16
BRL54443	詢價		廈門研科生物技術(shù)有限公司	2025-06-16
BRL-54443	詢價		武漢瓊格生物科技有限公司	2025-06-16
BRL54443	詢價		上海妍琦生物科技有限公司	2025-06-16
BRL 5444	￥2444		上海浩洋生物科技有限公司	2025-06-16
BRL54443	￥323		上海經(jīng)科化學(xué)科技有限公司	2025-06-16

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