20160614_商务部_2015药品流通行业运行统计分析.pdf
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1、MK-3207 HydrochlorideCat. No.: HY-10302CAS No.: 957116-20-0分式: CHClFNO分量: 594.05作靶点: CGRP Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (168.34 mM)* “ means soluble, but saturation unknown.Concentration
2、Solvent Mass 1 mg 5 mg 10 mg1 mM 1.6834 mL 8.4168 mL 16.8336 mL5 mM 0.3367 mL 1.6834 mL 3.3667 mL制备储备液10 mM 0.1683 mL 0.8417 mL 1.6834 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体内实验 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.21 mM); Clear solution1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% s
3、alineSolubility: 2.5 mg/mL (4.21 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.21 mM); Clear solution3. BIOLOGICAL ACTIVITY物活性 MK-3207 Hydrochloride 是种有效的,可服的 CGRP receptor 拮抗剂, IC50 值为 0.12 nM, Ki 值为 0.024 nM。IC n=14) as for human, but it 体外研究Product D
4、ata Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1displays 400-fold lower affinity for the canine and rat receptors, with values of 10 nM and 101.2 nM, respectively. MK-3207 is highly selective versus the human AM1 (CLR/RAMP2) and AM2 (CLR/RAMP3) receptors, with Ki values of 16,500 nM and
5、15617 nM, respectively. MK-3207 maintains a high degree of selectivity versus human CTR, with a Ki value of 1.90.58 M. MK-3207 also displays good selectivity versus the AMY3 (CTR/RAMP3) receptor, with a Ki value of 12825 nM, but it is less selective versus the AMY1 (CTR/RAMP1) receptor, with a Ki va
6、lue of 0.750.13 nM. MK-3207 potently blocks human -CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells, with an IC50 value of 0.120.02 nM. MK-3207 displays significantly lower potency for the rat CGRP receptor, with a pIC50=7.310.091.体内研究 MK-3207 is CNS-penetrant and theref
7、ore significantly engaging central receptors. After an oral dose of 10 mg/kg MK-3207, the CSF/plasma ratio is 2 to 3%1.PROTOCOLKinase Assay 1 Amylin binding assays are conducted by combining MK-3207 and 40 pM 125I-rat amylin, followed by 25 g of CTR/RAMP1 or 25 g of CTR/RAMP3 membranes and incubated
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