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- 2026年05月21日
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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
659730-32-2
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥660.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥272.0 |
| 规格： | 5 mg | 产品价格： | ￥600.0 |
| 规格： | 10 mg | 产品价格： | ￥1100.0 |
| 规格： | 25 mg | 产品价格： | ￥2500.0 |
| 规格： | 50 mg | 产品价格： | ￥4500.0 |
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AMG 517
CAS No. : 659730-32-2
MCE 国际站：AMG 517
产品活性：AMG 517是有效的香草素受体-1 (TRPV1) 拮抗剂，IC50值为0.5 nM。
研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点：TRP Channel
In Vitro: AMG 517 retains potency in the capsaicin- and acid-mediated assays with IC50 values of 0.9 and 0.5 nM. AMG 517 inhibits capsaicin, pH 5, and heat-induced45Ca2+ uptake into cells expressing TRPV1 with IC50 values of 1 to 2 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 ± 0.2 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.
In Vivo: AMG 517 is shown to be effective in a rodent “on-target” biochemical challenge model (capsaicin-induced flinch, ED50=0.33 mg/kg p.o.) and is antihyperalgesic in a model of inflammatory pain (CFA-induced thermal hyperalgesia, MED=0.83 mg/kg, p.o.).The minimally effective dose is 0.3 mg/kg for AMG 517 and the corresponding plasma concentration is 90 ng/mL. Oral administration of AMG 517 reverses established thermal hyperalgesia in a dose-dependent manner at 21 h after CFA injection. AMG 517 causes transient hyperthermia in rodents, dogs, and monkeys. AMG 517 induces hyperthermia in a steep dose-dependent manner, with 0.3, 1, and 3 mg/kg associated with 0.5, 0.6, and 1.6°C increases in body temperature, respectively. Body temperatures of rats treated with all doses of AMG 517 return to baseline within 10 to 20 h.
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文献和实验Silver Acetate Autometallography (AMG)
In the early eighties, a series of papers were published by Gorm DANSCHER, Aarhus, Denmark, to introduce a reliable and easy-to-handle technique for light microscopical and ultrastructural autometallographic (AMG) studies. Specific methods
Analysis of Yeast Telomerase by Primer Extension Assays
from this organism (Lendvay et al., Genetics 144:1399–1412, 1996). Moreover, much of the current understanding of the structure and function of the telomerase complex was derived from yeast studies (Autexier and Lue, Annu Rev Biochem 75:493–517, 2006
分子病理，选择分子靶向治疗。 RARP抑制剂成为卵巢癌个性化治疗的新宠。DNA修复PARP抑制剂奥拉帕尼作为靶向药物出现在2013年卵巢癌NCCN指南中。虽然FDA并未批准其用于卵巢癌的治疗，但PARP与BRCA1/2基因在DNA修复过程中的关系，使得PARP抑制剂成为卵巢癌个性化治疗的新宠。2012年发表在新英格兰杂志上的一篇报道，153位卵巢癌患者经过奥拉帕尼与安慰剂治疗比较，结果显示奥拉帕尼具有抗肿瘤活性，结果具有统计学意义。 抗血管类药物新成员AMG386。日前，欧盟已经批准
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