产品
编 号：F535447
分子式：C15H14N4S
分子量：282.36
分子式：C15H14N4S
分子量：282.36
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 949912-58-7
产品详情
生物活性：
Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model.
体内研究：
Remodelin (2 或 20 mg/kg，腹腔注射，每两天一次，持续 4 周) 显著降低肿瘤异种移植裸鼠模型中 AR 阴性前列腺癌的生长。Remodelin (100 mg/kg，口服) 在 LmnaG609G/G609G 小鼠早年衰老综合症 (HGPS) 模型中抑制 NAT10 并显著延长健康寿命。Remodelin (5 mg/kg，口服) 显示在小鼠中 T1/2 为 1.81 小时，口服生物利用度 (F%) 为 43.5%。 Pharmacokinetic parameters for Remodelin in MiceRouteDose (mg/kg)T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng/h/mL) AUC0-? (ng/h/mL) MRT_last (h) F(%)
p.o.51.810.254092352590.8443.5%
Animal Model:PC-3 cells tumor xenograft model in nude athymic BALB/c nu/nu mice
Dosage:2 or 20 mg/kg
Administration:Intraperitoneal injection (i.p.), once every two days for 4 weeks
Result:Significantly reduced AR-negative prostate cancer tumor growth.In the high-dose group, xenograft tumor weight at the endpoint was much smaller than that in the low-dose group.
Animal Model:LmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model
Dosage:100 mg/kg
Administration:Oral gavage (p.o.), daily schedule for 3 weeks of age onward, until the end-pointAmeliorated age-dependent weight loss.
Result:Ameliorated cardiac pathology.Led to the dramatic amelioration of HGPS cardiac pathologies, including reduction of adventitial fibrosis of the aorta, rescue of vascular smooth muscle cell loss, and salvage of smooth muscle actin (SMA) loss, both in the aorta and the coronary arteries.
Animal Model:WT Mice (Pharmacokinetic assay)
Dosage:5 mg/kg
Administration:Oral gavage (p.o.)
Result:Showed a T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice.
体外研究：
Remodelin (10-40 μM，1-7 天) 在 AR 阳性和 AR 阴性前列腺癌细胞中以剂量依赖性方式抑制 NAT10 活性和细胞增殖。Remodelin (20 μM，24 小时) 抑制前列腺癌细胞中的 NAT10 并减慢 DNA 复制。Remodelin (1 μM，7 天) 减少 LmnaG609G/G609G 成纤维细胞核形态缺陷并增加基因组稳定性。
Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model.
体内研究：
Remodelin (2 或 20 mg/kg，腹腔注射，每两天一次，持续 4 周) 显著降低肿瘤异种移植裸鼠模型中 AR 阴性前列腺癌的生长。Remodelin (100 mg/kg，口服) 在 LmnaG609G/G609G 小鼠早年衰老综合症 (HGPS) 模型中抑制 NAT10 并显著延长健康寿命。Remodelin (5 mg/kg，口服) 显示在小鼠中 T1/2 为 1.81 小时，口服生物利用度 (F%) 为 43.5%。 Pharmacokinetic parameters for Remodelin in MiceRouteDose (mg/kg)T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng/h/mL) AUC0-? (ng/h/mL) MRT_last (h) F(%)
p.o.51.810.254092352590.8443.5%
Animal Model:PC-3 cells tumor xenograft model in nude athymic BALB/c nu/nu mice
Dosage:2 or 20 mg/kg
Administration:Intraperitoneal injection (i.p.), once every two days for 4 weeks
Result:Significantly reduced AR-negative prostate cancer tumor growth.In the high-dose group, xenograft tumor weight at the endpoint was much smaller than that in the low-dose group.
Animal Model:LmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model
Dosage:100 mg/kg
Administration:Oral gavage (p.o.), daily schedule for 3 weeks of age onward, until the end-pointAmeliorated age-dependent weight loss.
Result:Ameliorated cardiac pathology.Led to the dramatic amelioration of HGPS cardiac pathologies, including reduction of adventitial fibrosis of the aorta, rescue of vascular smooth muscle cell loss, and salvage of smooth muscle actin (SMA) loss, both in the aorta and the coronary arteries.
Animal Model:WT Mice (Pharmacokinetic assay)
Dosage:5 mg/kg
Administration:Oral gavage (p.o.)
Result:Showed a T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice.
体外研究：
Remodelin (10-40 μM，1-7 天) 在 AR 阳性和 AR 阴性前列腺癌细胞中以剂量依赖性方式抑制 NAT10 活性和细胞增殖。Remodelin (20 μM，24 小时) 抑制前列腺癌细胞中的 NAT10 并减慢 DNA 复制。Remodelin (1 μM，7 天) 减少 LmnaG609G/G609G 成纤维细胞核形态缺陷并增加基因组稳定性。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备