产品
编 号：F142049
分子式：C29H23F6N5O3
分子量：603.52
分子式：C29H23F6N5O3
分子量：603.52
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 1374248-81-3
产品详情
生物活性：
Atogepant (MK-8031) is an orally active and selective calcitonin gene–related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
体内研究：
Atogepant (3, 10, 30 mg/kg; 口服; 每天一次; 9 天) 改善了硝酸甘油诱导大鼠面部异常性疼痛，和辣椒素诱导灵长类的真皮血管舒张。血浆、脑脊液和脑组织 (Sprague-Dawley 大鼠) 中 Atogepant 浓度和浓度比ParameterPlasma Cmax (ng/mL)CSF Cmax (ng/mL)Brain Cmax (ng/g)CSF/plasma Cmax ratios (ng/ml)Brain/plasma Cmax ratios (ng/ml)Brain/CSF Cmax ratios (ng/ml)Plasma AUC0-last (ng?h/ml)CSF AUC0-last (ng?h/ml)Brain AUC0-last (ng?h/g)CSF/plasma AUC0-last ratios (ng?h/ml)Brain/plasma AUC0-last ratios (ng?h/ml)Brain/CSF AUC0-last ratios (ng?h/ml)
Atogepant 5 mg/kg180.70.92.40.0050.01332.66671110.94.217.90.00380.01614.2619
Atogepant 20 mg/kg853.73.717.30.00430.02034.67576511.720.0102.30.00310.01575.1150
体外研究：
Atogepant 对人和非人 CGRP 受体的结合亲和力 (Ki, nM)SpeciesHuman (cloned)Human (native)RhesusRatMouseRabbitDog
K i (nM)0.0150.0260.0090.70.132.11.2
Atogepant对人类克隆的CGRP和相关受体具有功能性效能ReceptorCGRPAM1AM2CRTAMY1AMY3
IC50 (nM)0.026＞1800040062742.41418
Atogepant (MK-8031) is an orally active and selective calcitonin gene–related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
体内研究：
Atogepant (3, 10, 30 mg/kg; 口服; 每天一次; 9 天) 改善了硝酸甘油诱导大鼠面部异常性疼痛，和辣椒素诱导灵长类的真皮血管舒张。血浆、脑脊液和脑组织 (Sprague-Dawley 大鼠) 中 Atogepant 浓度和浓度比ParameterPlasma Cmax (ng/mL)CSF Cmax (ng/mL)Brain Cmax (ng/g)CSF/plasma Cmax ratios (ng/ml)Brain/plasma Cmax ratios (ng/ml)Brain/CSF Cmax ratios (ng/ml)Plasma AUC0-last (ng?h/ml)CSF AUC0-last (ng?h/ml)Brain AUC0-last (ng?h/g)CSF/plasma AUC0-last ratios (ng?h/ml)Brain/plasma AUC0-last ratios (ng?h/ml)Brain/CSF AUC0-last ratios (ng?h/ml)
Atogepant 5 mg/kg180.70.92.40.0050.01332.66671110.94.217.90.00380.01614.2619
Atogepant 20 mg/kg853.73.717.30.00430.02034.67576511.720.0102.30.00310.01575.1150
体外研究：
Atogepant 对人和非人 CGRP 受体的结合亲和力 (Ki, nM)SpeciesHuman (cloned)Human (native)RhesusRatMouseRabbitDog
K i (nM)0.0150.0260.0090.70.132.11.2
Atogepant对人类克隆的CGRP和相关受体具有功能性效能ReceptorCGRPAM1AM2CRTAMY1AMY3
IC50 (nM)0.026＞1800040062742.41418
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