
MK-3207 (Hydrochloride)
CAS No. 957116-20-0
MK-3207 (Hydrochloride) ( MK3207 Hydrochloride | MK 3207 Hydrochloride | MK-3207 )
产品货号. M16836 CAS No. 957116-20-0
一种高效、选择性 CGRP 受体拮抗剂,体外结合测定中的 Ki 为 21 pM,基于细胞的功能测定中的 IC50 为 0.12 nM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥1134 | 有现货 |
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10MG | ¥2074 | 有现货 |
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25MG | ¥3507 | 有现货 |
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50MG | ¥5646 | 有现货 |
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100MG | ¥8068 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称MK-3207 (Hydrochloride)
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述一种高效、选择性 CGRP 受体拮抗剂,体外结合测定中的 Ki 为 21 pM,基于细胞的功能测定中的 IC50 为 0.12 nM。
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产品描述A highly potent, selective CGRP receptor antagonist with Ki of 21 pM in in vitro binding assay and IC50 of 0.12 nM in cell-based functional assay; displays >50000-fold selectivity in a panel of 160 enzymes, receptors, channels, and 65-fold more potent than telcagepant; orally bioavailable.
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体外实验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 Ki values of 16,500 nM and 156±17 nM, respectively. MK-3207 maintains a high degree of selectivity versus human CTR, with a Ki value of 1.9±0.58 μM. MK-3207 also displays good selectivity versus the AMY3 (CTR/RAMP3) receptor, with a Ki value of 128±25 nM, but it is less selective versus the AMY1 (CTR/RAMP1) receptor, with a Ki value 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 IC50 value of 0.12±0.02 nM. MK-3207 displays significantly lower potency for the rat CGRP receptor, with a pIC50=7.31±0.09.
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体内实验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%.
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同义词MK3207 Hydrochloride | MK 3207 Hydrochloride | MK-3207
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通路GPCR/G Protein
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靶点CGRP Receptor
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受体CGRP
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研究领域Neurological Disease
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适应症——
化学信息
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CAS Number957116-20-0
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分子量594.0514
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分子式C31H30ClF2N5O3
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESC1CCC2(C1)C(=O)N(C(CN2)C3=CC(=CC(=C3)F)F)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4.Cl
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化学全称6,9-Diazaspiro[4.5]decane-9-acetamide, 8-(3,5-difluorophenyl)-10-oxo-N-[(2R)-1,1',2',3-tetrahydro-2'-oxospiro[2H-indene-2,3'-[3H]pyrrolo[2,3-b]pyridin]-5-yl]-, hydrochloride (1:1), (8R)-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Bell IM, et al. ACS Med Chem Lett. 2010 Jan 12;1(1):24-9.
2. Salvatore CA, et al. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60.
3. Li CC, et al. Br J Clin Pharmacol. 2015 May;79(5):831-7.
产品手册




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MK-3207
一种高效、选择性 CGRP 受体拮抗剂,体外结合测定中的 Ki 为 21 pM,基于细胞的功能测定中的 IC50 为 0.12 nM。