AF 12198
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:IL-1诱导的IL-8生成的IC50为25 nM.
IL-1α和IL-1β(白细胞介素-1)是炎症反应的有效调节剂.天然存在的白介素-1受体拮抗剂(IL-1ra)可以有效的调节体外和体内对IL-1的生物学应答.AF 12198是一种新型的低分子量IL-1拮抗剂.
体外实验:AF 12198与人I型IL-1受体选择性结合,不与人类II型受体或小鼠I型受体结合.AF 12198也抑制人皮肤成纤维细胞中IL-1诱导的IL-8的生成,IC50为25 nM.AF 12198可抑制内皮细胞IL-1诱导的细胞间粘附分子-1(ICAM-1)的表达,IC50为9 nM[2].
在体实验:食蟹猴静脉内注射AF 12198,阻断体内IL-1诱导的IL-6生成,下调体内诱导的IL-6.AF 12198是具有体内IL-1受体拮抗剂活性的第一个小分子拮抗剂[3].
临床试验:截至目前,AF 12198还处于临床前开发阶段.
参考文献：
[1] Akeson AL, Woods CW, Hsieh LC, Bohnke RA, Ackermann BL, Chan KY, Robinson JL, Yanofsky SD, Jacobs JW, Barrett RW, Bowlin TL. AF12198, a novel low molecular weight antagonist, selectively binds the human type I interleukin (IL)-1 receptor and blocks in vivo responses to IL-1. J Biol Chem. 1996 Nov 29;271(48):30517-23.
| Physical Appearance | White lyophilised solid |
| Storage | Desiccate at -20°C |
| M.Wt | 1895.12 |
| Cas No. | 185413-30-3 |
| Formula | C96H123N19O22 |
| Solubility | Soluble to 1 mg/ml in 10% ethanol/PBS |
| Chemical Name | (S,Z)-5-(((S,Z)-1-(((2S,3R)-1-((S)-2-((1Z,4Z,6S,7Z,9S,10Z,12S)-6-((1H-indol-3-yl)methyl)-1,4,7,10,15-pentahydroxy-12-((S)-2-((Z)-hydroxy(((S,Z)-1-hydroxy-1-(((S,Z)-1-hydroxy-1-(((S)-1-((S)-2-((Z)-hydroxy(((S)-1-hydroxy-1-imino-4-methylpentan-2-yl)imino)me |
| SDF | Download SDF |
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@]1([H])CCCN1C([C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@]2([H])CCN2C([C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@]3([H])CCCN3C([C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C)([H])CC4=CC=CC=C4)([H])CCC(O)=O)([H])CC5=CNC6= |
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化学结构
