化合物AMG517 T6379
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
25 mg | 659730-32-2 | ¥1,910.00 | 询底价 |
1 mg | 659730-32-2 | ¥221.00 | 询底价 |
100 mg | 659730-32-2 | ¥5,350.00 | 询底价 |
5 mg | 659730-32-2 | ¥493.00 | 询底价 |
10 mg | 659730-32-2 | ¥897.00 | 询底价 |
50 mg | 659730-32-2 | ¥3,720.00 | 询底价 |
1 mL | 659730-32-2 | ¥543.00 | 询底价 |
Product Introduction
Bioactivity
英文名: AMG 517
描述: AMG 517是一种有效的香草素受体-1 (TRPV1) 拮抗剂,IC50为0.5 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]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 43 mg/mL (100 mM)
关键字: Inhibitor | inhibit | Transient receptor potential channels | TRP Channel | AMG 517
相关产品: Pulegone | (-)-Menthol | JNJ-17203212 | A-967079 | NMDAR/TRPM4-IN-2 | TRPC6-PAM-C20 | MK6-83 | Adenosine 5'-diphosphoribose sodium | Vanilloid receptor antagonist 1 | D-GsMTx4 TFA
相关库: Ion Channel Inhibitor Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library
化合物AMG517 T6379信息由TargetMol中国为您提供,如您想了解更多关于化合物AMG517 T6379报价、型号、参数等信息,欢迎来电或留言咨询。
注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途