MK-2894
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.
MK-2894是一种高效的和选择性的EP4受体抑制剂,IC50值为2.5 nM[1].
MK-2894是一种高选择性的和强效的第二代EP4受体拮抗剂,在使用过表达人EP1-4 的HEK 293细胞系的细胞膜制备物的放射配体结合试验中,Ki值为0.56±0.1 nM.EP4 功能性试验测量MK-2894对PGE2诱导的cAMP积累的抑制,IC50值为2.5±0.7 nM.在雄性SD大鼠的AIA模型和胃肠耐受性模型中,MK-2894剂量依耐性抑制疼痛反应,ED50值为0.36 mg/kg.它还具有抑制慢性足肿胀的强效活性,ED50值为0.02 mg/kg/day.总的说来,MK-2894具有有待进一步发展所需的效力\选择性\药代动力学\以及胃肠道耐受特性,与传统的非甾体抗炎药(NSAIDs)和昔布类药物相比,在治疗疼痛和炎症中是潜在的更安全的替代物[1].
参考文献：
[1] Marc Blouin, Yongxin Han, Jason Burch, Julie Farand, Christophe Mellon, Mireille Gaudreault, Mark Wrona, Jean-Francois Levesque, Danielle Denis, Marie-Claude Mathieu, Rino Stocco, Erika Vigneault, Alex Therien, Patsy Clark, Steve Rowland, Daigen Xu, Gary O’Neill, Yves Ducharme and Rick Friesen. The Discovery of 4-{1-[({2,5-Dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic Acid (MK-2894), A Potent and Selective Prostaglandin E2 Subtype 4 Receptor Antagonist. J. Med. Chem. 2010, 53: 2227–2238.
| Storage | Store at -20°C |
| M.Wt | 473.51 |
| Cas No. | 1006036-87-8 |
| Formula | C25H22F3NO3S |
| Synonyms | MK 2894;MK2894 |
| Solubility | Soluble in DMSO |
| Chemical Name | 4-[1-[[2,5-dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]thiophene-3-carbonyl]amino]cyclopropyl]benzoic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C(=C(S1)C)C(=O)NC2(CC2)C3=CC=C(C=C3)C(=O)O)CC4=CC=C(C=C4)C(F)(F)F |
| 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。 |
| Description | MK-2894是一种高效的和选择性的EP4受体抑制剂,IC50值为2.5 nM. | |||||
| 靶点 | EP4 receptor | |||||
| IC50 | 2.5 nM (Ki=0.56±0.1 nM??/td> | |||||
化学结构
