CAY10618

生物活性靶点体外研究体内研究 CAY10618 试剂级价格

CAY10618

CAS号:1202580-59-3
英文名:CAY10618
中文名:CAY10618
CBNumber:CB42590444
分子式:C27H29N5O
分子量:439.55
MOL File:1202580-59-3.mol

CAY10618化学性质

密度 :1.15±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
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

CAY10618性质、用途与生产工艺

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.