RS 127445
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.
RS-127445（MT 500）是5-HT2B受体的选择性拮抗剂，其pKi和pIC50值分别为9.5和10.4[1]。
5-HT2B受体属于5-HT2受体家族，结合神经递质血清素。5-HT2B在血清素相关反应中起着重要作用，包括神经敏感到触觉刺激。
RS-127445是血清素5-HT2B受体的选择性抑制剂。据发现，RS-127445对5-HT2B受体具有纳摩尔的亲和性和1000倍的选择性[2]。RS-127445有效地阻断5-HT诱导的肌醇磷酸增加，并阻止5-HT诱导的细胞内钙浓度增加，比Yohimbine作用于细胞内钙浓度的效能高1000倍。
在大鼠模型中，给予1 ~ 10 mg/kg的RS-127445显著抑制高达35 ~ 74%的应激引发的内脏高敏感性[3]。此外，3 ~ 30 mg/kg的RS-127445显著抑制15 ~ 62%的由TNBS诱导的内脏高敏感性[3]。
参考文献：
[1]. O'Mahony, S M et al. 5-HT2B receptors modulate visceral hypersensitivity in a stress-sensitive animal model of brain-gut axis dysfunction. Neurogastroenterology & Motility, 2012, 22(5): 573-578.
[2]. Ohashi-Doi K et al. A selective, high affinity 5-HT2B receptor antagonist inhibits visceral hypersensitivity in rats. Neurogastroenterology & Motility, 2010, 22(2): 69-76.
[3]. Bassil A K et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. British Journal of Pharmacology, 2009, 158(1): 252-258.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 281.33 |
| Cas No. | 199864-87-4 |
| Formula | C17H16FN3 |
| Synonyms | RS-127445; MT 500; RS127445 |
| Solubility | insoluble in H2O; ≥15.89 mg/mL in DMSO; ≥20.07 mg/mL in EtOH |
| Chemical Name | 4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine |
| SDF | Download SDF |
| Canonical SMILES | FC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=CC=CC=C31 |
| 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 | RS 127445是高亲和力的5-HT2B受体拮抗剂，其pKi值为9.5。 | |||||
| 靶点 | 5-HT2B receptor | |||||
| IC50 | 9.5 (pKi) | |||||
质量控制和MSDS
- 批次:
化学结构
