产品
编 号：F756562
分子式：C36H44N4O4S
分子量：628.82
分子式：C36H44N4O4S
分子量：628.82
产品类型
规格
价格
是否有货
结构图
CAS No: 2881068-33-1
产品详情
生物活性：
DPTIP-proagent 18 (P18) is a orally active and brain-penetrable proagent of DPTIP (HY-131002). DPTIP-proagent 18 is a potent nSMase2 inhibitor. DPTIP-proagent 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-proagent 18 can be used for brain injury research.
体内研究：
DPTIP-prodrug 18 exhibits an excellent PK profile. DPTIP-prodrug 18 shows significant inhibition of nSMase2 activity and IL-1β-induced EV release in mice.Animal Model:CES1–/– mice
Dosage:10 mg/kg DPTIP equivalent
Administration:Orally, once (Pharmacokinetic Analysis)
Result:Exhibited >fourfold higher plasma (AUC0-t=1047 pmol·h/mL) and brain exposures (AUC0-t=247 pmol·h/g) versus DPTIP and a significant enhancement of DPTIP half-life (2 h vs ~0.5 h).
Animal Model:Interleukin-1β-injected mice (a mouse model of brain injury)
Dosage:0, 3 and 10 mg/kg (DPTIP equivalent)
Administration:Orally, once
Result:Significantly inhibited the release of brain-derived GFP+ EVs into the blood at both 3 and 10 mg/kg (DPTIP equivalent dose).
体外研究：
DPTIP-prodrug 18 is metabolically stable with >75% intact prodrug remaining after 1 h of incubation at 37 °C.
DPTIP-proagent 18 (P18) is a orally active and brain-penetrable proagent of DPTIP (HY-131002). DPTIP-proagent 18 is a potent nSMase2 inhibitor. DPTIP-proagent 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-proagent 18 can be used for brain injury research.
体内研究：
DPTIP-prodrug 18 exhibits an excellent PK profile. DPTIP-prodrug 18 shows significant inhibition of nSMase2 activity and IL-1β-induced EV release in mice.Animal Model:CES1–/– mice
Dosage:10 mg/kg DPTIP equivalent
Administration:Orally, once (Pharmacokinetic Analysis)
Result:Exhibited >fourfold higher plasma (AUC0-t=1047 pmol·h/mL) and brain exposures (AUC0-t=247 pmol·h/g) versus DPTIP and a significant enhancement of DPTIP half-life (2 h vs ~0.5 h).
Animal Model:Interleukin-1β-injected mice (a mouse model of brain injury)
Dosage:0, 3 and 10 mg/kg (DPTIP equivalent)
Administration:Orally, once
Result:Significantly inhibited the release of brain-derived GFP+ EVs into the blood at both 3 and 10 mg/kg (DPTIP equivalent dose).
体外研究：
DPTIP-prodrug 18 is metabolically stable with >75% intact prodrug remaining after 1 h of incubation at 37 °C.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备