1202580-59-3

中文名称 CAY10618

英文名称 CAY10618

CAS 1202580-59-3

分子式 C27H29N5O

分子量 439.55

MOL 文件 1202580-59-3.mol

1202580-59-3 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T15412

英文别名

GPP 78
CAY10618
CAY10618 Exclusive
N-(2-phenylphenyl)-8-(4-pyridin-3-yltriazol-1-yl)octanamide
1H-1,2,3-Triazole-1-octanaMide, N-[1,1'-biphenyl]-2-yl-4-(3-pyridinyl)-

物理化学性质

密度1.15±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml; Ethanol: 10 mg/ml

酸度系数(pKa)14.80±0.70(Predicted)

形态Liquid

颜色Colorless to light yellow

常见问题列表

生物活性

GPP78 (CAY10618) 是一种有效的烟酰胺磷酸核糖转移酶 (Nampt) 抑制剂，对 NAD 消耗的 IC50 为 3 nM。GPP78 通过诱导自噬对神经母细胞瘤细胞 SH-SY5Y 具有毒性，IC50 为 3.8 nM。GPP78 具有抗癌和抗炎作用。

靶点

Nampt;
Autophagy

体外研究

GPP78 (Compound 8; 10 nM; 24-40 hours; SH-SY5Y cells) treatment with cells, punctate staining of LC3-II and the formation of autophagolysosomes are observable. LC3-II is membrane-bound and is present in autophagosomes.
GPP78 (Compound 8) inhibits the growth of most cell lines tested, with nanomolar potency (GI ₅₀ ) in cell lines derived from leukemia, lung, CNS, colon, melanoma, ovarian, renal, and prostate cancers. GPP78 appears truly cytotoxic in melanoma cell lines, while in the others it is mainly cytostatic.

Western Blot Analysis

Cell Line:	SH-SY5Y cells
Concentration:	10 nM
Incubation Time:	24 hours, 40 hours
Result:	Punctate staining of LC3-II and the formation of autophagolysosomes were observable.

体内研究

GPP78 (10 mg/kg; intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days; male adult CD1 mice) treatment reduces the severity of spinal cord trauma in SCI mice.

Animal Model:	Male adult CD1 mice (25-30 g) with spinal cord injury (SCI)
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days
Result:	Significantly reduced the demyelination associated with SCI. And significantly ameliorated the functional deficits induced by SCI.