AMD 3465
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.
通过GTP结合测得其对CXCR4活化的IC50值为10.38 ± 1.99 nM.
CXCR4在多种细胞类型中广泛表达,参与新生儿发育\造血作用\淋巴细胞运输和归巢.另外,CXCR4是HIV的共受体,因而CXCR4的小分子拮抗剂具有治疗潜力.AMD 3465是N-吡啶基乙烯单环拉胺类CXCR4拮抗剂,抑制T细胞嗜性的\使用CXCR4的HIV感染.
体外实验:在表达CXCR4的CCRF-CEM T细胞系中,AMD3465是SDF-1配体结合的拮抗剂,抑制SDF-1介导的信号通路,包括抑制GTP结合和钙流及抑制趋化作用.AMD3465并不抑制表达CXC3\CCR1\CCR2b\CCR4\CCR5或CCR7的细胞中趋化因子诱导的钙流,也不抑制LTB4与其受体BLT1结合[1].
体内试验:小鼠和狗皮下注射AMD3465能够引起白细胞增多,动员高峰出现在小鼠皮下注射后0.5至1.5小时,狗中动员高峰前出现化合物的最大峰值血浆浓度,表明AMD3465具有动员造血干细胞的潜能.这些数据表明CXCR4拮抗剂AMD3465具有治疗潜能[1].
临床试验:目前尚无临床数据.
参考文献：
[1] Bodart V, Anastassov V, Darkes MC, Idzan SR, Labrecque J, Lau G, Mosi RM, Neff KS, Nelson KL, Ruzek MC, Patel K, Santucci Z, Scarborough R, Wong RS, Bridger GJ, Macfarland RT, Fricker SP. Pharmacology of AMD3465: a small molecule antagonist of the chemokine receptor CXCR4. Biochem Pharmacol. 2009;78(8):993-1000.
| Storage | Store at -20°C |
| M.Wt | 410.6 |
| Cas No. | 185991-24-6 |
| Formula | C24H38N6 |
| Solubility | Soluble in DMSO |
| Chemical Name | N-(pyridin-2-ylmethyl)-1-[4-(1,4,8,11-tetrazacyclotetradec-1-ylmethyl)phenyl]methanamine |
| SDF | Download SDF |
| Canonical SMILES | C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CNCC3=CC=CC=N3 |
| 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。 |
