| 产品描述： | MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC50=0.12 nM; Ki=0.024 nM). MK-3207 can be used for migraine studies |
| 靶点： |
CGRP Receptor |
| 体内研究： |
MK-3207 (0.3, 0.6, 2.1, 9.1, 21.2, 60.6 µg/kg; i.v.; single) inhibits CIDV in rhesus monkeys with EC50 and Emax values of approximately 0.8 nM and 81%. MK-3207 (10 mg/kg; p.o.; single) shows the CSF/plasma ratio is 2 to 3%. Animal Model: Adult rhesus monkeys (4.8-12.7 kg; capsaicin-induced). Dosage: 0.3, 0.6, 2.1, 9.1, 21.2, 60.6 µg/kg Administration: Intravenous injection; single. Result: Resulted in an exposure-dependent decrease in capsaicin-induced dermal vasodilation in the rhesus monkey forearm. |
| 参考文献： |
1. Salvatore CA, Moore EL, Calamari A, Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.793 ml |
8.967 ml |
17.934 ml |
| 5 mM |
0.359 ml |
1.793 ml |
3.587 ml |
| 10 mM |
0.179 ml |
0.897 ml |
1.793 ml |
| 50 mM |
0.036 ml |
0.179 ml |
0.359 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京