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NBI-27914 hydrochloride

更新时间:2025-08-27 13:50:02

NBI-27914 hydrochloride结构式
NBI-27914 hydrochloride结构式
品牌特惠专场
常用名 NBI-27914 hydrochloride 英文名 NBI 27914 hydrochloride
CAS号 1215766-76-9 分子量 470.651
密度 N/A 沸点 N/A
分子式 C18H21Cl5N4 熔点 N/A
MSDS N/A 闪点 N/A

 NBI-27914 hydrochloride用途


NBI-27914(盐酸盐)是一种选择性促肾上腺皮质激素释放因子1(CRF1)受体拮抗剂,Ki值为1.7 nM[1][3][4]。

 NBI-27914 hydrochloride名称

英文名 5-Chloro-N-(cyclopropylmethyl)-2-methyl-N-propyl-N'-(2,4,6-trichlorophenyl)-4,6-pyrimidinediamine hydrochloride (1:1)
英文别名 更多

 NBI-27914 hydrochloride生物活性

描述 NBI-27914(盐酸盐)是一种选择性促肾上腺皮质激素释放因子1(CRF1)受体拮抗剂,Ki值为1.7 nM[1][3][4]。
相关类别
靶点实验

Ki: 1.7 nM (CRF1 receptor)[4]

体内研究 NBI 27914(3~30 mg/kg;i.p.)盐酸盐可在最高试验剂量下减轻所述腹痛,在吲哚美辛给药后4小时和24小时均有效[1]。NBI 27914(1~10 mg/kg;i.p.)盐酸盐剂量依赖性地减轻弗氏完全佐剂诱导的机械性痛觉过敏。NBI 27914(10 mg/kg)盐酸盐逆转热痛觉过敏。NBI 27914盐酸盐分别以5和10 mg/kg的最小有效剂量减弱脊神经结扎引起的机械性痛觉过敏和触觉性痛觉超敏[1]。较高剂量的NBI 27914盐酸盐可阻断行为性癫痫发作,并防止杏仁核记录的并发脑电图中的癫痫放电[2]。动物模型:雄性CD-1小鼠(20~25g)[1]剂量:3~30mg/kg给药:I.p.结果:在最高试验剂量下,消炎痛给药后4和24h均有效。
参考文献

[1]. Peng YL, et al. Central Neuropeptide S inhibits food intake in mice through activation of Neuropeptide S receptor. Peptides. 2010;31(12):2259-2263.

[2]. Hummel M, et al. Pain is a salient "stressor" that is mediated by corticotropin-releasing factor-1 receptors. Neuropharmacology. 2010;59(3):160-166.

[3]. Baram TZ, et al. The CRF1 receptor mediates the excitatory actions of corticotropin releasing factor (CRF) in the developing rat brain: in vivo evidence using a novel, selective, non-peptide CRF receptor antagonist. Brain Res. 1997;770(1-2):89-95.

[4]. Chen C, et al. Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists. J Med Chem.

 NBI-27914 hydrochloride物理化学性质

分子式 C18H21Cl5N4
分子量 470.651
精确质量 468.020874
InChIKey CPMGENCTAWBLNW-UHFFFAOYSA-N
SMILES CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1Cl.Cl

 NBI-27914 hydrochloride靶点实验

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实验名称:Cell-based high throughput primary assay to identify activators of GPR151
来源:The Scripps Research Institute Molecular Screening Center
靶标:RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL
External Id:GPR151_PHUNTER_AG_LUMI_1536_1X%ACT
实验名称:AlphaScreen-based biochemical high throughput primary assay to identify activators of...
来源:The Scripps Research Institute Molecular Screening Center
靶标:N/A
External Id:FBW7_ACT_ALPHA_1536_1X%ACT PRUN
实验名称:AlphaScreen-based biochemical high throughput primary assay to identify inhibitors of...
来源:The Scripps Research Institute Molecular Screening Center
External Id:MITF_INH_Alpha_1536_1X%INH PRUN
实验名称:Tocris HTS for Inhibitors of Aerobactin Synthetase lucA
来源:23265
External Id:IucA Pilot Assay Tocris Library
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 NBI-27914 hydrochloride英文别名

4,6-Pyrimidinediamine, 5-chloro-N4-(cyclopropylmethyl)-2-methyl-N4-propyl-N6-(2,4,6-trichlorophenyl)-, hydrochloride (1:1)
5-Chloro-N-(cyclopropylmethyl)-2-methyl-N-propyl-N'-(2,4,6-trichlorophenyl)-4,6-pyrimidinediamine hydrochloride (1:1)
MFCD05662281
5-Chloro-N-(cyclopropylmethyl)-2-methyl-N-propyl-N'-(2,4,6-trichlorophenyl)pyrimidine-4,6-diamine hydrochloride (1:1)
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