AMG-517
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.
AMG-517是TRPV1通道的拮抗剂,IC50值为1-2 nM [1]。
TRPV1,瞬时受体电位阳离子通道亚家族V成员1,属于瞬时受体电位蛋白亚家族,在检测和调节体温及传感疼痛中起重要作用。TRPV1可以被各种刺激激活,包括一些炎性成分,可造成疼痛和灼热感。据报道,TRPV1通道可以在许多疾病中发挥关键作用,如SIRS [1,2]。
AMG-517是TRPV1的拮抗剂。在稳转TRPV1的CHO细胞系中, AMG-517抑制TRPV1的激活[1]。
在LPS诱导的全身炎症反应综合征的C57BL / 6小鼠中,AMG-517(210 g/kg)预处理显著降低存活率,增加死亡风险[2]。在TRPV1敲除小鼠中,腹腔给药AMG-517(256 nmol/kg)以剂量依赖的方式抑制热疗诱导的TRPV1 激活[3]。在辣椒素诱导的退缩雄性Sprague-Dawley大鼠中,口服给药AMG-517以剂量依赖性方式显著减少退缩的次数[1]。
参考文献:
[1]. Gavva, N.R., et al., Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther, 2007. 323(1): p. 128-37.
[2]. Wanner, S.P., et al., Aging reverses the role of the transient receptor potential vanilloid-1 channel in systemic inflammation from anti-inflammatory to proinflammatory. Cell Cycle, 2012. 11(2): p. 343-9.
[3]. Garami, A., et al., Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia. J Neurosci, 2010. 30(4): p. 1435-40.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 430.4 |
Cas No. | 659730-32-2 |
Formula | C20H13F3N4O2S |
Solubility | ≥21.5 mg/mL in DMSO; insoluble in H2O; ≥4.93 mg/mL in EtOH |
Chemical Name | N-[4-[6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl]oxy-1,3-benzothiazol-2-yl]acetamide |
SDF | Download SDF |
Canonical SMILES | CC(=O)NC1=NC2=C(C=CC=C2S1)OC3=NC=NC(=C3)C4=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。 |
细胞实验[1]: | |
细胞系 |
CHO细胞 |
溶解方法 |
在DMSO中的溶解度大于21.5mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
1-2 nM |
应用 |
AMG 517是一个选择性的人和大鼠TRPV1拮抗剂,对人和大鼠的解离常数分别为4.2和6.2 nM。在体外,AMG 517能够有效地和完全地抑制辣椒素、质子和热激活的TRPV1。在表达TRPV1的CHO细胞中,AMG 517有效地抑制辣椒素、酸和热诱导的Ca2+摄取,IC50为1-2 nM。 |
临床实验[2]: | |
临床样本 |
健康成年人 |
剂量 |
口服给药,2、5和10 mg |
应用 |
在健康成年人中,AMG 517抑制TRPV1活性,引发血药浓度依赖的体温过高。AMG 517通过增加产热和尾皮肤血管收缩,导致体温过高,表明在人类中TRPV1可调控代谢产热和血管张力。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Gavva N R, Bannon A W, Hovland D N, et al. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 323(1): 128-137. [2]. Gavva N R, Treanor J J S, Garami A, et al. Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans[J]. Pain, 2008, 136(1): 202-210. |
Description | AMG-517 is a highly selective antagonist of TRPV1 with IC50 values of 0.76 nM, 0.62 nM and 1.3 nM for capsaicin-, proton- and heat-induced inward currents, respectively. | |||||
Targets | capsaicin-induced inward currents | proton-induced inward currents | heat-induced inward currents | |||
IC50 | 0.76 nM | 0.62 nM | 1.3 nM |
质量控制和MSDS
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