價(jià)格 | ¥525 | ¥762 | ¥1230 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-09-29 |
中文名稱:化合物 BCATc Inhibitor 2 | 英文名稱:BCATc Inhibitor 2 |
CAS:406191-34-2 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 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: 98.80% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T22043 |
名稱 | BCATc Inhibitor 2 |
描述 | BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective efficacy in vivo[1]. Branched-chain amino acid transferases (BCATs) have been implicated in catalyzing reversible transamination of isoleucine, leucine, and valine branched-chain amino acids to their corresponding α-keto acids, generating L-glutamate. It has been identified that there are two forms of BCAT in mammals: mitochondrial BCAT (BCATm) and cytosolic BCAT (BCATc). BCATc is expressed in particular brain region and involved in regulating glutamate synthesis for release during neuronal excitation. Thus, BCATc inhibition may be useful for the treatment of neurodegenerative and behavioral disorders involving disturbances of the glutamatergic system [2]. |
體外活性 | BCATc抑制劑可能有助于治療涉及谷氨酸系統(tǒng)紊亂的神經(jīng)退行性及其他神經(jīng)障礙。在hBCATc實(shí)驗(yàn)中,BCATc Inhibitor 2的IC50值為0.8 ± 0.05 μM。在重組大鼠BCATc實(shí)驗(yàn)和粗制大鼠BCATm實(shí)驗(yàn)中,其IC50分別為0.2 μM ± 0.02和3.0 μM ± 0.5(n=5)。BCATc Inhibitor 2在神經(jīng)細(xì)胞培養(yǎng)中減少了鈣離子流入,IC50為4.8 ± 1.2 μM(n=4)[1]。 |
體內(nèi)活性 | BCATc Inhibitor 2在抑制谷氨酸攝取后阻斷了鈣離子流入神經(jīng)細(xì)胞,并在體內(nèi)顯示出神經(jīng)保護(hù)效果。在Lewis大鼠中,經(jīng)30 mg/kg BCATc Inhibitor 2(皮下注射)處理后,血漿峰值濃度(Cmax)在0.5小時(shí)(tmax)達(dá)到8.28 μg/ml。平均血漿暴露量(AUC)值為19.9 μg h/ml,平均末端半衰期介于12至15小時(shí),表明BCATc Inhibitor 2具有有利的藥代動(dòng)力學(xué)(PK)參數(shù)。每日給予線粒體神經(jīng)毒素3-硝基丙酸(3-NP)產(chǎn)生紋狀體損害并導(dǎo)致運(yùn)動(dòng)缺陷。連續(xù)9天給藥的BCATc Inhibitor 2幾乎完全逆轉(zhuǎn)了3-NP的效應(yīng)[1]。 |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 65 mg/ml (155.22 mM) |
關(guān)鍵字 | cytosolic | neurodegenerative | human | BCATc Inhibitor-2 | mitochondrial | disease | rBCATc | BCATc Inhibitor 2 | Inhibitor | BCAT | rBCATm | inhibit | hBCATc | BCATc Inhibitor2 |
相關(guān)庫(kù) | 神經(jīng)保護(hù)化合物庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | NO PAINS 化合物庫(kù) |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)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(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
產(chǎn)品名稱 | 價(jià)格 | 公司名稱 | 報(bào)價(jià)日期 | |
---|---|---|---|---|
詢價(jià) |
VIP2年
|
陜西締都新材料有限公司
|
2024-11-06 | |
詢價(jià) |
VIP10年
|
上海昭昀生物科技有限公司
|
2024-11-12 | |
詢價(jià) |
VIP3年
|
上海嘉定區(qū)澄瀏公路52號(hào)
|
2024-11-12 |