mavatrep
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.
Mavatrep是一种有效的和口服可用的TRPV1拮抗剂,其IC50值为4.6 nM[1][2].
瞬时受体电位香草酸亚型1(TRPV1)是一种热敏性与非选择性的阳离子通道,属于TRP通道超家族.该通道由酸性pH(< 6.8)\热刺激(> 43 ℃)以及内源性脂类介质(花生四烯酸乙醇胺及亚油酸氧化代谢物)激活[1].
Mavatrep是一种有效的和口服可用的TRPV1拮抗剂.在稳定表达人或大鼠TRPV1(rTRPV1)通道的HEK293细胞中,Mavatrep(1 μM)抑制Capsaicin诱导的Ca2+内流,其IC50值分别为4.6 nM和21 nM.在全细胞膜片钳电生理实验中,Mavatrep呈浓度依赖性地抑制pH(5.0)与Capsaicin(1 μM)激活的hTRPV1通道,其IC50值分别为6.8 nM和23 nM.此外,Mavatrep(0.1 μM)也抑制74 ± 8.1%的hTRPV1介导的热诱发电流[1].
在CFA炎性疼痛模型中,Mavatrep(10 mg/kg,口服)显著地逆转CFA诱导的热超敏,其ED50值和ED80值分别为1.8 mg/kg和7.8 mg/kg[1].
参考文献:
[1]. Parsons WH, Calvo RR, Cheung W, et al. Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). J Med Chem, 2015, 58(9): 3859-3874.
Storage | Store at -20°C |
M.Wt | 422.44 |
Cas No. | 956274-94-5 |
Formula | C25H21F3N2O |
Solubility | Soluble in DMSO |
Chemical Name | (E)-2-(2-(2-(4-(trifluoromethyl)styryl)-1H-benzo[d]imidazol-6-yl)phenyl)propan-2-ol |
SDF | Download SDF |
Canonical SMILES | CC(C1=CC=CC=C1C2=CC(N3)=C(N=C3/C([H])=C([H])/C4=CC=C(C(F)(F)F)C=C4)C=C2)(O)C |
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。 |