品牌咨询
联系方式
公司地址
苏州工业园区生物纳米园A4#216
联系电话
4000-520-616 / 18915418616
传真号码
0512-67156496
电子邮箱
info@ebiomall.com
公司网址
https://www.ebiomall.com
商品描述
AMG517
- Catalog No.：MC0301
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 659730-32-2
- MolecularFormula：
- C20H13F3N4O2S
- Purity：
- >98%
- Target：
- TRP Channel
- IC50：
- IC50: 0.5 nM (TRPV1)[1]
- In Vitro：
- AMG 517 retains potency in the capsaicin- and acid-mediated assays with IC50 values of 0.9 and 0.5 nM[1]. 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[2].
- 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.)[1].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[2].
- Fields：
- AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM.
- Specificity：
- Target:TRP Channel. Fields: AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM.
- Source：
- Rabbit
- Dilution：
- IC50: 0.5 nM (TRPV1)[1]
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- AMG517; AMG-517
- MolecularWeight(Da)：
- 430.4
- References：
- [1]. Doherty EM, et al. Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J Med Chem. 2007 Jul 26;50(15
- June 19-2018
- WESTERN IMMUNOBLOTTING PROTOCOL
- June 19-2018
- IMMUNOHISTOCHEMISTRY-PARAFFIN PROTOCOL
- June 19-2018
- IMMUNOFLUORESCENCE PROTOCOL
- September 08-2020
- FLOW-CYTOMEYRT-PROTOCOL
- July 13-2018
- CELL-BASED-ELISA-PROTOCOL-FOR-ACETYL-PROTEIN
- July 13-2018
- CELL-BASED-ELISA-PROTOCOL-FOR-PHOSPHO-PROTEIN
- July 13-2018
- CELL-BASED-COLORIMETRIC-ELISA-PROTOCOL-FOR-TOTAL-PROTEIN
- July 13-2018
- Antibody-FAQs
- Products Images
