化合物 JTC801|T6553|TargetMol

價格	￥255	￥417
包裝	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

QQ交談微信洽談

產(chǎn)品詳情

中文名稱:化合物 JTC801	英文名稱:JTC-801
CAS:244218-51-7	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.27%	產(chǎn)品類別: 抑制劑
貨號: T6553

Product Introduction

Bioactivity

名稱	JTC-801
描述	JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
激酶實(shí)驗(yàn)	A suspension of membranes from human μ-opioid receptor-expressing CHO-K1 cells in 50 mM Tris-HCl buffer (pH 7.4) containing 5 mM MgCl2 and 10% sucrose is incubated at room temperature for 2.5 h with 0.33 nM 3H-labeled diprenorphine and various concentrations of JTC-801. The membranes are collected by filtration using Whatman 934-AH, and radioactivity is counted with a TopCount A9912V scintillation counter. Nonspecific binding (6.4%) is determined with 10 μM naloxone. Specific binding is calculated by subtracting nonspecific binding from the total binding. Data are the mean±SE (n=3).
體外活性	JTC-801 displays about 12.5-, 129-, and 1055-fold selectivity for ORL1 receptor (Ki = 8.2 nM) over μ-, κ-, and δ-opioid receptors, respectively. JTC-801 does not inhibit forskolin-stimulated cyclic AMP accumulation in human ORL1 receptor-expressing HeLa cells, but it prevents nociceptin-induced inhibition of cyclic AMP accumulation, indicating that JTC-801 possesses full antagonistic activity. [2] In rat cerebrocortical membrane, JTC-801 inhibits ORL1 receptor with IC50 of 472 nM and μ-receptor with IC50 of 1831 nM. JTC-801 completely antagonizes the suppression of nociceptin on forskolin-induced accumulation of cyclic AMP with IC50 of 2.58 μM in HeLa cells expressing ORL1 receptor. [1]
體內(nèi)活性	Oral administration of JTC-801 (0.3-3 mg/kg) antagonizes nociceptin-induced allodynia in mice, and shows analgesic effect in a hot plate test using mice and in a formalin test using rats. [2] In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL) or exposed heat stimulus with minimum effective doses (MED) of 0.01 mg/kg by i.v. or 1 mg/kg by p.o. In the rat formalin test, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01 mg/kg71 by i.v. or 1 mg/kg by p.o. [1] JTC-801 dose-dependently normalizes paw withdrawal latency (PWL). Although JTC-801 does not inhibit a chronic constriction injury (CCI)-induced decrease in bone mineral content (BMC) and bone mineral density (BMD), it inhibits an increase in the number of osteoclasts. [3] Tactile allodynia induced by L5/L6 spinal nerve ligation is reversed by both systemic (3-30 mg/kg) and spinal (22.5 and 45 pg) JTC-801 in a dose-dependent manner. Furthermore, systemic JTC-801 reduces Fos-like immunoreactivity in the dorsal horn of the spinal cord (laminae I/II). [4] JTC-801 produces dose-dependent mechanical and cold anti-allodynic effects with ED50 of 0.83 mg/kg and 1.02 mg/kg, respectively. [6]
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 44.8 mg/mL (100 mM) Ethanol : 9 mg/mL (20 mM)
關(guān)鍵字	Opioid Receptor \| Inhibitor \| inhibit \| JTC-801
相關(guān)產(chǎn)品	Docusate sodium \| Progesterone \| Naltrexone hydrochloride \| SCH 221510 \| Matrine \| Amentoflavone \| Mirtazapine \| Mianserin hydrochloride \| (-)-Menthol \| Bevenopran \| Naloxone HCl Dihydrate \| Trimebutine
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| GPCR靶點(diǎn)分子庫 \| 膜蛋白靶向化合物庫 \| 神經(jīng)退行性疾病化合物庫 \| 疼痛相關(guān)化合物庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字： N-(4-氨基-2-甲基-6-喹啉基)-2-[(4-乙基苯氧基)甲基]苯甲酰胺鹽酸鹽|||JTC801|||JTC 801|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計算機(jī)輔助藥物設(shè)計）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊資本	566.265100萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 3年

公司成立：12年
注冊資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號8樓

進(jìn)入店鋪

詢盤

店內(nèi)推薦

化合物 2-(Chloromethyl)-3,5-dimethyl-4-nitropyridine|T65985|TargetMol

詢價

2,4-二甲基吡咯-3,5-二羧酸二乙酯|T77705|TargetMol

￥100

化合物 cis-4-(Aminomethyl)cyclohexanecarboxylic acid|T67148|TargetMol

詢價