AR-M 1896
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.
结合IC50:rGalR2的IC50为1.76 nM, hGalR1的IC50为879 nM.
Galanin(甘丙肽)是一种含有29个氨基酸的神经肽,在疼痛处理中具有复杂的作用.甘丙肽受体亚型存在于背根神经节和脊髓中,具有不同的分布.已鉴定并克隆三种甘丙肽受体GALR1\GALR2和GALR3.AR-M1896是一个特异的甘丙肽R2(GALR2)受体激动剂.
体外实验:去除位置1的甘氨酸残基对AR-M1896对GALR2的亲和力和功能性活性没有影响,与GalR1-Rs相比,对GalR2-Rs具有500倍的选择性.该化合物代表一个真正的GalR2选择性的甘丙肽类似物,因此,可以用作药理学工具对两种受体进行区分[1].
在体实验:在正常大鼠中,鞘内输注低剂量的甘丙肽,诱导后爪的机械和冷异常性疼痛.等摩尔剂量的AR-M1896或AR-M961诱导产生相同的效果,其分别是GALR1和GALR2受体的激动剂.在异常性疼痛Bennett大鼠模型中,鞘内注射高剂量的AR-M961后,机械阈值剂量依赖性增加,但在AR-M1896对照组没有观察到任何效果.在非异常性疼痛Bennett大鼠模型中,没有观察到任一化合物的作用[1].
临床试验:截至目前,AR-M1896还处于临床前开发阶段.
参考文献：
[1] Liu HX, Brumovsky P, Schmidt R, Brown W, Payza K, Hodzic L, Pou C, Godbout C, Hkfelt T.
Receptor subtype-specific pronociceptive and analgesic actions of galanin in the spinal cord: selective actions via GalR1 and GalR2 receptors. Proc Natl Acad Sci U S A. 2001 Aug 14;98(17):9960-4.
| Physical Appearance | White lyophilised solid |
| Storage | Desiccate at -20°C |
| M.Wt | 1136.31 |
| Cas No. | 367518-31-8 |
| Formula | C54H81N13O14 |
| Solubility | Soluble to 1 mg/ml in 20% formic acid |
| SDF | Download SDF |
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC1=CNC2=CC=CC=C12)([H])[C@@](O)([H])C)([H])CC(C)C)([H])CC(O)=N)([H])CO)([H])C)([H])CC3=CC=C(O)C=C3)([H])CC(C)C)([H])C(O)=N)C |
| 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。 |
化学结构
