2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. DPTIP-prodrug 18

DPTIP-prodrug 18  (Synonyms: P18)

目录号: HY-149025
产品使用指南

摩尔计算器

DPTIP-prodrug 18 (P18) 是一种口服有效的、可透过血脑屏障的 DPTIP (HY-131002) 前体活性分子。DPTIP-prodrug 18 是一种有效的中性鞘磷脂酶 nSMase2 抑制剂。DPTIP-prodrug 18 通过抑制 nSMase2 活性，显著抑制 IL-1β 诱导的膜泡 (EV) 释放。DPTIP-prodrug 18 可用于脑损伤研究。

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DPTIP-prodrug 18 Chemical Structure

DPTIP-prodrug 18 Chemical Structure

CAS No. : 2881068-33-1

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DPTIP-prodrug 18 相关抗体

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查看 Phospholipase 亚型特异性产品:

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Phospholipase A PLD Phospholipase C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

nSMase2[1]
体外研究
(In Vitro)

DPTIP-prodrug 18 is metabolically stable with >75% intact prodrug remaining after 1 h of incubation at 37 °C[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DPTIP-prodrug 18 相关抗体:
体内研究
(In Vivo)

DPTIP-prodrug 18 exhibits an excellent PK profile[1].
DPTIP-prodrug 18 shows significant inhibition of nSMase2 activity and IL-1β-induced EV release in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CES1–/– mice[1]
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)[1]
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).
Clinical Trial
分子量

628.82

Formula

C36H44N4O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DPTIP-prodrug 18 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DPTIP-prodrug 182881068-33-1P18P 18P-18PhospholipaseNeutral sphingomyelinase-2nSMase2IL-1βbrain injuryorally activebrain-penetrableInhibitorinhibitorinhibit

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