BRL-54443

價(jià)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?jiān)L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(diǎn)	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(shí)驗(yàn)	?
特征	?

推薦的實(shí)驗(yàn)操作(此推薦來自于公開的文獻(xiàn)所以Selleck并不保證其有效性)

激酶實(shí)驗(yàn): ^[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(shí)驗(yàn): ^[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?duì)I業(yè)額
主營行業(yè)		經(jīng)營模式

Selleck中國

非會員

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(bào)價(jià)

產(chǎn)品名稱	價(jià)格		公司名稱	報(bào)價(jià)日期
3-(1-甲基哌啶-4-基)-1H-吲哚-5-醇 57477-39-1	詢價(jià)	VIP5年	河南威梯?；た萍加邢薰?/div>	2025-02-08
BRL-54443	￥890		上海晶抗生物工程有限公司	2025-01-30
BRL-54443	￥729.21		上海超研生物科技有限公司	2025-01-30
BRL-54443	￥756		上海意杰生物科技有限公司	2025-01-30
aladdin 阿拉丁 B129734 BRL-54443,5-HT 1E和5-HT 1F受體激動劑 57477-39-1 ≥98%	￥35.90	VIP13年	上海阿拉丁生化科技股份有限公司	2025-01-20
化合物 BRL54443\|T2459\|TargetMol	￥183	VIP12年	上海陶術(shù)生物科技有限公司	2024-12-02
aladdin 阿拉丁 B409219 BRL-54443 57477-39-1 10mM in DMSO	￥957.90	VIP2年	上海阿拉丁生化科技股份有限公司	2024-11-29
3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇	詢價(jià)		湖北新迪科化學(xué)有限公司	2024-07-24
BRL-54443	詢價(jià)		上海禾午生物科技有限公司	2020-11-03
BRL-54443	￥370		上海嶸崴達(dá)實(shí)業(yè)有限公司	2020-01-16

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