CAS NO: | 957116-20-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | MK-3207 (Hydrochloride) is a potent and orally bioavailableCGRP receptorantagonist withIC50of 0.12 nM andKiof 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3. | ||||||||||||||||
IC50& Target | IC50: 0.12 nM (CGRP receptor) | ||||||||||||||||
体外研究 (In Vitro) | MK-3207 displays a similar affinity (Ki) for the rhesus monkey receptor (0.024±0.001 nM; n=14) as for human, but it displays >400-fold lower affinity for the canine and rat receptors, with values of 10 nM and 10±1.2 nM, respectively. MK-3207 is highly selective versus the human AM1 (CLR/RAMP2) and AM2 (CLR/RAMP3) receptors, with Kivalues of 16,500 nM and 156±17 nM, respectively. MK-3207 maintains a high degree of selectivity versus human CTR, with a Kivalue of 1.9±0.58 μM. MK-3207 also displays good selectivity versus the AMY3 (CTR/RAMP3) receptor, with a Kivalue of 128±25 nM, but it is less selective versus the AMY1 (CTR/RAMP1) receptor, with a Kivalue of 0.75±0.13 nM. MK-3207 potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells, with an IC50value of 0.12±0.02 nM. MK-3207 displays significantly lower potency for the rat CGRP receptor, with a pIC50=7.31±0.09[1]. | ||||||||||||||||
体内研究 (In Vivo) | MK-3207 is CNS-penetrant and therefore significantly engaging central receptors. After an oral dose of 10 mg/kg MK-3207, the CSF/plasma ratio is 2 to 3%[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 594.05 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C31H30ClF2N5O3 | ||||||||||||||||
CAS 号 | 957116-20-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(168.34 mM) H2O : 50 mg/mL(84.17 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液
* 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。 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
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