Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-3207 Hydrochloride (MK-3207 HCl) 是口服具有活力的CGRP receptor 拮抗剂,IC50=0.12 nM,Ki=0.024 nM。
产品描述 | MK-3207 Hydrochloride (MK-3207 HCl) is a potent CGRP receptor antagonist with IC50 and Kiof 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. Phase 2. |
靶点活性 | CGRP:0.12 nM |
体外活性 | MK 3207 exhibits significantly higher affinity for both native and recombinant human CGRP receptor, as well as rhesus monkey CGRP receptor with Ki of 24 pM, ~24 pM and 22 pM, respectively, as compared to CGRP receptors from other species, including canine and rodent (Ki values of ~10 nM). Although has affinity for AMY1 (CTR/RAMP1) receptor with a Ki value of 0.75 nM, MK 3207 displays marked selectivity for human CGRP receptor versus related human AM1 (CLR/RAMP2) receptor, AM2 (CLR/RAMP3) receptor, AMY3 (CTR/RAMP3) receptor, and CTR with Ki values of 16.5 μM, 0.156 μM, 0.128 μM and 1.9 μM, respectively. MK 3207 potently inhibits human α-CGRP-induced cAMP production in HEK293 cells stably expressing human CLR/RAMP1 with an IC50 of 0.12 nM, and maintains similar potency in the presence of 50% human serum with an IC50 of 0.17 nM, indicating that the activity of MK 3207 would not be dramatically affected by plasma protein binding in vivo. MK 3207 exhibits approximately 65-fold more potent in the human serum-shifted in vitro functional assay than telcagepant with an IC50 of 10.9 nM. [1] |
体内活性 | Administration of MK 3207 produces a concentration-dependent inhibition of capsaicin-induced dermal vasodilation in rhesus monkeys, blocking the blood flow increase with an EC50 of 0.8 nM and an EC90 of 7 nM, respectively. MK 3207 displays approximately 100-fold more potent in the rhesus monkey CIDV assay versus telcagepant with an EC90 of 994 nM. [1] |
激酶实验 | Amylin binding assays are conducted by combining MK-3207 and 40 pM 125I-rat amylin, followed by 25 μg of CTR/RAMP1 or 25 μg of CTR/RAMP3 membranes and incubated for 3 h at room temperature in binding buffer (10 mM HEPES, 5 mM MgCl2, and 0.2% bovine serum albumin) in a total volume of 1 mL. Calcitonin binding assays are with 25 μg of CTR membranes and 30 pM 125I-human calcitonin as the radioligand. Incubations are terminated by filtration through GF/B 96-well filter plates that has been blocked with 0.5% polyethylenimine. Data are analyzed using Prism, and the Ki value is determined using the equation Ki=IC50/1 + ([ligand]/KD). The KD value for each receptor is determined by saturation binding experiments. |
别名 | MK-3207 HCl |
分子量 | 594.05 |
分子式 | C31H29F2N5O3·HCl |
CAS No. | 957116-20-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 119 mg/mL (200.31 mM)
H2O: 5 mg/mL (8.41 mM)
DMSO: 119 mg/mL (200.31 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / H2O / DMSO | 1 mM | 1.6834 mL | 8.4168 mL | 16.8336 mL | 42.084 mL |
5 mM | 0.3367 mL | 1.6834 mL | 3.3667 mL | 8.4168 mL | |
Ethanol / DMSO | 10 mM | 0.1683 mL | 0.8417 mL | 1.6834 mL | 4.2084 mL |
20 mM | 0.0842 mL | 0.4208 mL | 0.8417 mL | 2.1042 mL | |
50 mM | 0.0337 mL | 0.1683 mL | 0.3367 mL | 0.8417 mL | |
100 mM | 0.0168 mL | 0.0842 mL | 0.1683 mL | 0.4208 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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