MK-3207 是一种口服有效的、具有高选择性和种属特异性的CGRP受体拮抗剂 (对人CGRP受体:IC50=0.12 nM;Ki=0.024 nM)。MK-3207 可用于偏头痛的研究。
生物活性 | MK-3207 is an orally active, highly selective and species-specificCGRP receptorantagonist (for humanCGRP receptor:IC50=0.12 nM;Ki=0.024 nM). MK-3207 can be used for migraine studies[1]. |
体外研究 (In Vitro) | 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[1].
Cell Viability Assay[1] Cell Line: | HEK293 cells (stably expressing human CLR/RAMP1) | Concentration: | 0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM | Incubation Time: | 30 min (pre-treat) | Result: | Blocked human α-CGRP-stimulated cAMP responses with an IC50value of 0.12 nM. |
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体内研究 (In Vivo) | 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 EC50and Emaxvalues of approximately 0.8 nM and 81%[1]. MK-3207 (10 mg/kg; p.o.; single) shows the CSF/plasma ratio is 2 to 3%[1].
Animal Model: | Adult rhesus monkeys (4.8-12.7 kg; capsaicin-induced)[1]. | 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)[1]. | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : ≥ 150 mg/mL(269.01 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.7934 mL | 8.9672 mL | 17.9343 mL | 5 mM | 0.3587 mL | 1.7934 mL | 3.5869 mL | 10 mM | 0.1793 mL | 0.8967 mL | 1.7934 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.48 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.48 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.48 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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