Sograzepide (Synonyms: Netazepide; YF 476; YM-220)
目录号: PL04279 纯度: ≥98%
CAS No. :155488-25-8
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中文名称
Sograzepide
中文别名
N-[(3R)-1-(3,3-二甲基-2-氧代丁基)-2,3-二氢-2-氧代-5-(2-吡啶基)-1H-1,4-苯并二氮杂卓-3-基]-N'-[3-(甲基氨基)苯基]脲;N-苄氧羰基-L-谷氨酸-5-苄脂
英文名称
Sograzepide
英文别名
N-[(3R)-1-(3,3-Dimethyl-2-oxobutyl)-2,3-dihydro-2-oxo-5-(2-pyridinyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]urea;1-[(3R)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-pyridin-2-yl-3H-1,4-benzodiazepin-3-yl]-3-[3-(methylamino)phenyl]urea;Sograzepide;(R)-1-[2,3-Dihydro-2-oxo-1-pivaloylmethyl-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl]-3-(3-methylaminophenyl)urea;1-[(3R)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-pyridin-2-yl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]-3-[3-(methylamino)phenyl]urea;Urea,N-[1-(3,3-dimethyl-2-oxobutyl)-2,3-dihydro-2-oxo-5-(2-pyridinyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]-,(R)-;YF 476;Estradiol-3-O-sulfamate
Cas No.
155488-25-8
分子式
C28H30N6O3
分子量
498.58
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Sograzepide (Netazepide; YF 476; YM-220) 是一种非常有效,高选择性和口服活性的 Gastrin/CCK-B 拮抗剂,IC50 值为 0.1 nM,还抑制 Gastrin/CCK-A 活性, IC50 值 为 502 nM。Sograzepide (Netazepide; YF 476; YM-220) 取代 [125I]CCK-8 与大鼠脑,克隆犬和人 Gastrin/CCK-B 的特异性结合,Ki 值分别为 0.068、0.62 和 0.19 nM。
生物活性
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC 50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC 50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with K i values of 0.068, 0.62 and 0.19 nM, respectively.
性状
Solid
IC50 & Target[1][2]
IC50: 0.1 nM (Gastrin/CCK-B); 501 nM (Gastrin/CCK-A)
体内研究(In Vivo)
Sograzepide (Netazepide; YF 476; YM-220) (0.1 μmol/kg; intravenous injection) has an inhibition effect on pentagastrin-induced gastric acid secretion in anethsetized rats with an ED 50 of 87?nmol/kg.
Sograzepide (Netazepide; YF 476; YM-220) (intravenous injection; 10 μM/kg) inhibits pentagastrin-induced acid secretion with an ED 50 value of 0.0086 μM/kg, but does not affect histamine- and bethanechol-induced acid secretion.
Sograzepide (Netazepide; YF 476; YM-220) (intravenous injection; oral administration) in Heidenhain pouch dogs, inhibits pentagastrin-stimulated gastric acid secretion in a dose-dependent manner with ED 50 values of 0.018 and 0.020 μM/kg, respectively . has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Boyce M, et al. Effect of netazepide, a gastrin/CCK2 receptor antagonist, on gastric acid secretion and rabeprazole-induced hypergastrinaemia in healthy subjects. Br J Clin Pharmacol. 2015 May;79(5):744-55.
[2]. Takinami Y, et al. YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo.Aliment Pharmacol Ther. 1997 Feb;11(1):113-20.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (200.57 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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