RQ-00203078
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:对hTRPM8和rTRPM8的IC50分别为8.3和5.8 nM.
瞬时受体电位melastatin 8(TRPM8)是TRP melastatin亚家族的成员,在疾病引起的冷痛觉过敏和冷异常性疼痛中发挥重要作用,如奥沙利铂\长春新碱或紫杉醇等化疗引起的周围神经病变(CIPN)\糖尿病性神经病以及偏头痛和膀胱过度活动症(OAB).RS-00203078是TRPM8的选择性拮抗剂,具有口服活性.
体外实验:在薄荷醇诱导的钙内流实验中,RQ-00203078是一种新型的和高效的TRPM8拮抗剂,在人和大鼠中的IC50分别为8.3和5.8 nM.与其它TRP通道相比,RQ-00203078对TRPM8具有高选择性[1].
在体实验:RQ-00203078具有极好的体内活性,在icilin诱导的猛烈震颤大鼠模型中,口服给药RQ-00203078以剂量依赖的方式产生活性,ED50值为0.65 mg/kg[1].
临床试验:到目前为止,RQ-00203078还处于临床前开发阶段.
参考文献:
[1] Ohmi M, Shishido Y, Inoue T, Ando K, Fujiuchi A, Yamada A, Watanabe S, Kawamura K. Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 554.85 |
Cas No. | 1254205-52-1 |
Formula | C21H13ClF6N2O5S |
Solubility | insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥27.25 mg/mL in EtOH |
Chemical Name | 4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid |
SDF | Download SDF |
Canonical SMILES | ClC1=C(N(CC2=CC=C(OC(F)(F)F)C=C2)S(C3=CC=C(C(O)=O)C=C3)(=O)=O)N=CC(C(F)(F)F)=C1 |
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。 |
质量控制和MSDS
- 批次:
化学结构
![RQ-00203078](http://www.apexbt.com//media/diy/images/struct/B5872.png)