RQ-00203078
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.
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
