产品
编 号：F539332
分子式：C31H29F2N5O3
分子量：557.59
分子式：C31H29F2N5O3
分子量：557.59
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 957118-49-9
产品详情
生物活性：
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.
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.
Animal Model:Adult rhesus monkeys (4.8-12.7 kg).
Dosage:10 mg/kg
Administration:Oral administration; single.
Result:Exhibited the CSF/plasma ratio was 2 to 3%, however the CSF/plasma ratio was approximately 30% of the unbound fraction (9.4%) in plasma.
体外研究：
MK-3207 (0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM; 30 min) potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells.
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.
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.
Animal Model:Adult rhesus monkeys (4.8-12.7 kg).
Dosage:10 mg/kg
Administration:Oral administration; single.
Result:Exhibited the CSF/plasma ratio was 2 to 3%, however the CSF/plasma ratio was approximately 30% of the unbound fraction (9.4%) in plasma.
体外研究：
MK-3207 (0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM; 30 min) potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells.
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