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产品名称
TLR4抑制剂，TAK-242, TAK-242; CAS 243984-11-4; is a cell-permeable compound that selectively binds to Cys747 of TLR4 and selectively disrupts its interaction with adaptor molecules TIRAP and TRAM.
品質等級
化驗
≥98% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
white to yellow-white
溶解度
DMSO: 100 mg/mL
運輸包裝
wet ice
儲存溫度
2-8°C
InChI
1S/C15H17ClFNO4S/c1-2-22-15(19)11-5-3-4-6-14(11)23(20,21)18-13-8-7-10(17)9-12(13)16/h5,7-9,14,18H,2-4,6H2,1H3/t14-/m1/s1
InChI 密鑰
LEEIJTHMHDMWLJ-CQSZACIVSA-N
一般說明
一种细胞渗透性环己烯羧酸盐，可通过TLR4细胞内Cys747残基选择性的结合TLR4而非TLR1-3或TLR5-10，破坏TLR4与衔接子分子TIRAP和TRAM的相互作用。已显示出可有效抑制TLR4介导的信号转导事件，包括在鼠RAW264.7巨噬细胞中LPS诱导的NO和炎性细胞因子生成（针对NO、IL-6和TNF-α生成的各自IC50 = 1.8，1.3和1.9 nM）、TLR4/TIRAP依赖性NF-κB活性以及在TIRAP或TRAM转染的HEK293-hTLR4/MD2-CD14细胞中的TLR4/TIRAP-和TLR4/TRAM依赖性ISRE活性(IC50<300 nM)。据报道，静脉注射给药3 mg/kg时，TAK-242可完全抑制小鼠体内LPS（7 mg/kg，腹腔注射）诱导的死亡。与头孢他啶（3 mg/kg TAK-242和20 mg/kg头孢他啶，i.v.）共同给药时，因感染性休克而导致的死亡的彻底消除可扩展至活的大肠杆菌感染的小鼠。
一种细胞渗透性环己烯羧酸盐，可通过与TLR4细胞内Cys747残基的直接结合TLR4，而非TLR1-3或TLR5-10，与衔接子分子TIRAP和TRAM的相互作用。已显示出在体外可有效抑制TLR4介导的信号转导事件（针对在鼠RAW264.7巨噬细胞中LPS诱导的NO、IL-6和TNF-α生成分别的IC50 = 1.8，1.3和1.9 nM），以及在小鼠（3 mg/kg；i.v.）体内完全阻止LPS-（7 mg/kg，i.p.）诱导的死亡。还可以提供在DMSO（货号508336）中的25 mM溶液。
生化／生理作用
可逆性：是
细胞可渗透性：具有
首要靶标
TLR4
TLR4
包裝
用惰性气体包装
警告
毒性：有害（C）
重構
在重悬后分装并冻存于冰箱（-70°C）。储备液可在-70°C最长稳定1年。仅使用新鲜的DMSO。
其他說明
Matsunaga, N., et al. 2011.Mol.Pharmacol.79, 34.
Takashima, K., et al. 2009.Br. J. Pharmacol.157, 1250.
Li, M., et al. 2006.Mol.Pharmacol.69, 1288.
Yamada, M., et al. 2005.J. Med. Chem.48, 7457.
Takashima, K., et al. 2009.Br. J. Pharmacol.157, 1250.
Li, M., et al. 2006.Mol.Pharmacol.69, 1288.
Yamada, M., et al. 2005.J. Med. Chem.48, 7457.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 2
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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