AT 56
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.
PGD24是参与睡眠和炎症反应的脂质介质.PGD2激活两种不同类型的受体.在中枢神经系统中,PGD2通过DP1受体调节睡眠和疼痛.该前列腺素还经由DP1受体引起气道平滑肌的收缩,通过外围DP2受体介导嗜酸性粒细胞和嗜碱性粒细胞进入肺的趋化性.因此,PGD2通过这两种受体协调过敏性反应,尤其是气道炎症.AT-56是脂质运载蛋白型前列腺素D合成酶的具有口服活性的选择性抑制剂.
体外实验:3-250 μM的AT-56以浓度依赖性方式抑制人和小鼠L-PGDS,但不影响造血PGD合酶(H-PGDS)\环加氧酶1和2以及微粒PGE合酶1.AT-56与底物PGH2(Km=14 μM)竞争性抑制L-PGDS的活性, Ki值为75 μM,不抑制13-顺式视黄酸这种非底物的亲脂性配体与L-PGDS的结合[2].
在体实验:在H-PGDS缺陷型小鼠脑中,刺伤损伤后,小于30 mg/kg的AT-56口服给药,以剂量依赖性方式将脑中PGD2的产量下降到40%,但不影响PGE2和PGF2α的生成.在人L-PGDS转基因小鼠抗原诱发的肺部炎症模型中,AT-56抑制支气管肺泡灌洗液中嗜酸性粒细胞和单核细胞的累积[3].
临床试验:到目前为止,AT-56仍处于临床前开发阶段.
参考文献:
[1] Daisuke Irikura, Kosuke Aritake, Nanae Nagata, Toshihiko Maruyama, Shigeru Shimamoto, and Yoshihiro Urade. Biochemical, Functional, and Pharmacological Characterization of AT-56, an Orally Active and Selective Inhibitor of Lipocalin-type Prostaglandin D Synthase. J Biol Chem. 2009 Mar 20;284(12):7623-30.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 397.52 |
Cas No. | 162640-98-4 |
Formula | C25H27N5 |
Solubility | Soluble in DMSO |
Chemical Name | 1-(4-(2H-tetrazol-5-yl)butyl)-4-(5H-dibenzo[a,d][7]annulen-5-ylidene)piperidine |
SDF | Download SDF |
Canonical SMILES | N(CC/1)(CCCCC2=NNN=N2)CCC1=C3C4=CC=CC=C4C=CC5=CC=CC=C\35 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |