GRA Ex-25
目录号: PL05080 纯度: ≥98%
CAS No. :307983-31-9
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中文名称
GRA Ex-25
中文别名
(2S)-4-(2,5-二氟苯基)-N-[(3R,4S)-3-氟-1-甲基-4-哌啶基]-2,5-二氢-2-羟基甲基-N-甲基-2-苯基-1H-吡咯-1-羧胺;N-[4-[[[反式-4-(1,1-二甲基乙基)环己基][[[4-(三氟甲氧基)苯基]氨基]羰基]氨基]甲基]苄基]-B-丙氨酸
英文名称
GRA Ex-25
英文别名
b-Alanine,N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-;B-ALANINE, N-[4-[[[TRANS-4-(1,1-DIMETHYLETHYL)CYCLOHEXYL][[[4-(TRIFLUOROMETHOXY)PHENYL]AMINO]CARBONYL]AMINO]METHYL]BENZ...;GRA Ex-25;B-Alanine,N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]
Cas No.
307983-31-9
分子式
C29H36N3O5F3
分子量
563.61
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GRA Ex-25 是一种 glucagon 受体的抑制剂,抑制大鼠和人的 glucagon 受体,IC50 值分别为 56 和 55 nM。
生物活性
GRA Ex-25 is an inhibitor of glucagon receptor, with IC 50 of 56 and 55 nM for rat and human glucagon receptors, respectively.
性状
Solid
IC50 & Target[1][2]
IC50: 56 nM (rat glucagon receptor), 55 nM (human glucagon receptor)
体外研究(In Vitro)
GRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with Ki of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with Ki of 254 nM under our assay conditions. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GRA Ex-25 (3 mg/kg, i.v.) significantly reduces blood glucose caused by exogenous administration of glucagon in rat model. GRA Ex-25 is able to inhibit the rise in blood glucose levels elicited by exogenous administered glucagon, most likely because of the direct inhibition of glucagon stimulated hepatic glucose output. 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
参考文献
[1]. Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50.
[2]. Lau J, et al. New beta-alanine derivatives are orally available glucagon receptor antagonists. J Med Chem. 2007 Jan 11;50(1):113-28.
溶解度数据
In Vitro: DMSO : ≥ 32 mg/mL (56.78 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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