NMDA receptor antagonist 2,NMDA receptor antagonist 2

NMDA receptor antagonist 2|T40999|TargetMol

價格	￥10600
包裝	25mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-30

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產(chǎn)品詳情

中文名稱:NMDA receptor antagonist 2	英文名稱:NMDA receptor antagonist 2
CAS:875898-41-2	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.
產(chǎn)品類別: 抑制劑
貨號: T40999

Product Introduction

Bioactivity

名稱	NMDA receptor antagonist 2
描述	NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits remarkable binding affinities, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound finds valuable application in scientific investigations focusing on neuropathic pain and Parkinson’s disease.
體外活性	NMDA receptor antagonist 2 leads to excellent potency at NR2B (K i =0.88 nM) and selectivity over hERG binding (IP=20000 nM). NMDA receptor antagonist 2 is evaluated in a functional assay measuring Ca 2+ flux in cells expressing recombinant NR1/NR2B receptors. Selectivity over the hERG-channel is evaluated in an MK-499-binding assay[1].NMDA receptor antagonist 2 is highly potent in a functional assay using cells expressing NR2B (IC 50 =1.0 nM) and remains equipotent in a binding assay using a sample of homogenized human temporal cortex (K i =0.81 nM). In an electrophysiology assay using NR2B receptors,?Compound 22?shows full blockade of ion flux with?K D =0.35 nM. Compound?22?also exhibits high levels of selectivity over NR2A (IC 50 =200 μM), hERG binding (IP=20 μM), α-adrenergic receptors based on Prazosin binding (IC 50 >100 μM),?and CYP P450s including CYP3A4, 2C9, and 2D6[1].
體內(nèi)活性	In pharmacokinetic studies with higher species, NMDA receptor antagonist 2 shows excellent oral bioavailability (F=83%), half-life (T 1/2 =7.5 hours) and clearance (CL=3.6 mL/min/kg) in dog. And it exhibits moderate clearance (CL=12 mL/min/kg) and oral bioavailability (F=17%) in rhesus, the half-life (T 1/2 ) is 1.5 hours[1]. In a rat pharmacokinetic study, NMDA receptor antagonist 2 shows oral bioavailability (F=23 %), half-life (T 1/2 =0.7 hours) and clearance (CL=24 mL/min/kg), the receptor occupancy ED 50 with oral administration is 4.8 mg/kg in rat[1]. In the spinal nerve ligation model of neuropathic pain in rats, surgical ligation of two lumbar nerves in the spinal column induces a state of mechanical allodynia[1].NMDA receptor antagonist 2 (oral administration; 3-30 mg/kg) inhibits tactile allodynia in a dose-dependent manner after oral administration at 10 and 30 mg/kg. It produces an average improvement in the maximal possible effect of 15% (3 mg/kg), 41% (10 mg/kg), and 69% (30 mg/kg) compared to vehicle treated animals[1].NMDA receptor antagonist 2 (oral administration; 3-30 mg/kg) is efficacious in an acute rodent model of Parkinson’s disease. Haloperidol (HY-14538) is administered at a dose previously shown to elicit an acute cataleptic response in rats, compound 22 reduces catalepsy scores in a dose-dependent manner, producing average improvements of 34% (3 mg/kg), 86% (10 mg/kg), and 92% (30 mg/kg) when it compares to vehicle group[1].
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
關(guān)鍵字	NMDA receptor antagonist 2

關(guān)鍵字： NMDA receptor antagonist 2|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（計算機輔助藥物設(shè)計）研究中心、藥理實驗室、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	589.8595萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,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)

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公司成立：12年
注冊資本：589.8595萬人民幣
企業(yè)類型：有限責任公司(自然人投資或控股)
主營產(chǎn)品：抑制劑&激動劑，天然產(chǎn)物，重組蛋白，化合物庫，技術(shù)服務(wù)
公司地址：上海市靜安區(qū)江場三路238號8樓

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