Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AMG 517是一种有效的香草素受体-1 (TRPV1) 拮抗剂,IC50为0.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 221 | 现货 | ||
5 mg | ¥ 493 | 现货 | ||
10 mg | ¥ 897 | 现货 | ||
25 mg | ¥ 1,910 | 现货 | ||
50 mg | ¥ 3,720 | 现货 | ||
100 mg | ¥ 5,350 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 543 | 现货 |
产品描述 | AMG 517 is an effective and specific TRPV1 antagonist, antagonizes proton (IC50: 0.76 nM), capsaicin (IC50: 0.62 nM), and heat activation (IC50: 1.3 nM) of TRPV1. |
靶点活性 | TRPV1(capsaicin):0.62 nM, TRPV1(heat activation):1.3 nM, TRPV1(proton):0.76 nM |
体外活性 | AMG 517 inhibits CAP- (500 nM), acid- (pH 5.0), or heat-(45 °C) induced 45Ca2+ influx into human TRPV1-expressing CHO Cells with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. AMG 517 blocks capsaicin-, proton-, and heat-induced inward currents in TRPV1-expressing cells similarly. AMG 517 inhibits native TRPV1 activation by capsaicin in rat dorsal root ganglion neurons with an IC50 value of 0.68 nM. AMG 517 is a competitive antagonist of both rat and human TRPV1 with dissociation constant (Kb) values of 4.2 and 6.2 nM, respectively. AMG 517 is a highly selective TRPV1 antagonist. The IC50 value for AMG 517 is >20 μM against 2-APB-activated TRPV2 and TRPV3, 4-αPDD-activated TRPV4, allyl isothiocyanate-activated TRPA1, and icilin-activated TRPM8 in cell-based assays that measure agonist-induced increases in intracellular calcium in CHO cells recombinantly expressing the appropriate TRP channel. [1] |
体内活性 | Oral administration of AMG 517 produces a dose-dependent increase in plasma concentrations, it also produces a dose-dependent decrease in the number of flinches induced by capsaicin treatment. The minimally effective dose (MED), based on a statistically significant difference in number of flinches from the vehicle versus capsaicin-administered group, is 0.3 mg/kg for AMG 517. The corresponding plasma concentrations are 90 to 100 ng/mL for AMG 517. AMG 517 (3 mg/kg) exhibits significant reductions in capsaicin-induced flinch up to 24 h after dosing. AMG 517 blocks thermal hyperalgesia in CFA model of pain.[1] AMG 517 elicits hyperthermia in rodents, dogs and monkeys but not in TRPV1 knockout mice. Interestingly, hyperthermia evoked by TRPV1-selective antagonists is attenuated after repeated dosing of these antagonists to rats, dogs and monkeys, and TRPV1 knockout mice does not exhibit an impairment of thermoregulation.[2] |
别名 | AMG517, N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺, AMG-517 |
分子量 | 430.4 |
分子式 | C20H13F3N4O2S |
CAS No. | 659730-32-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 43 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3234 mL | 11.6171 mL | 23.2342 mL | 58.0855 mL |
5 mM | 0.4647 mL | 2.3234 mL | 4.6468 mL | 11.6171 mL | |
10 mM | 0.2323 mL | 1.1617 mL | 2.3234 mL | 5.8086 mL | |
20 mM | 0.1162 mL | 0.5809 mL | 1.1617 mL | 2.9043 mL | |
50 mM | 0.0465 mL | 0.2323 mL | 0.4647 mL | 1.1617 mL | |
100 mM | 0.0232 mL | 0.1162 mL | 0.2323 mL | 0.5809 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AMG 517 659730-32-2 Membrane transporter/Ion channel TRP/TRPV Channel AMG517 Inhibitor inhibit Transient receptor potential channels N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺 TRP Channel AMG-517 inhibitor