1. Vitamin D Related/Nuclear Receptor
  2. Progesterone Receptor
  3. EIDD-1723

EIDD-1723 是一种 Progesterone (HY-N0437) 类似物,可与孕酮受体 (PR) 结合,其 IC50 为 2.25 μM。EIDD-1723 是 EIDD-036 (HY-17649) 的前药。EIDD-1723 可能不仅通过孕酮受体 (PR) 依赖性途径发挥神经保护作用,还可能通过非基因组机制发挥神经保护作用,例如调节炎症反应和氧化应激。EIDD-1723 可用于创伤性脑损伤 (TBI) 的研究。

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EIDD-1723

EIDD-1723 Chemical Structure

CAS No. : 1659302-89-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EIDD-1723 is a Progesterone (HY-N0437) analogues, that binds progesterone receptor (PR) with an IC50 of 2.25 μM. EIDD-1723 is the prodrug of EIDD-036 (HY-17649). EIDD-1723 may exert its neuroprotective effects not solely through progesterone receptor (PR)-dependent pathways but also via non-genomic mechanisms, such as modulation of inflammatory responses and oxidative stress. EIDD-1723 can be used for the study of traumatic brain injury (TBI)[1][2][3].

体外研究
(In Vitro)

ANT308 (1-10 μM, 48 h) 显著增强 CD4+ 和 CD8+ T 细胞中 CD69 和 Ki67 的表达[1]

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

药代动力学
(Parmacokinetics)[2]
Species Dose Route Indicator value
Rat 10 mg/kg i.m. Cmax 1362 ng/mL
Rat 2 mg/kg i.v. Cmax 182 ng/mL
Rat 10 mg/kg i.m. AUClast 724 ng·h/mL
Rat 2 mg/kg i.v. AUClast 48 ng·h/mL
体内研究
(In Vivo)

EIDD-1723 (3-30 mg/kg,肌肉注射;2 mg/kg,静脉注射;30 mg/kg,口服,单剂量) 肌肉注射后可迅速完全转化为活性代谢物 EIDD-036,该代谢物能够穿过血脑屏障[1][3]
EIDD-1723 (10 mg/kg,肌肉注射,共 9 次) 可显著减少大鼠脑水肿,并改善运动、感觉和空间学习障碍的恢复[1][3]

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

Animal Model: TBI model induced by controlled cortical impact (CCI) established in male SD rats weighing 200-350 g[1][3]
Dosage: 10 mg/kg
Administration: Intramuscular injection (i.m.), at 1, 6, and 24 h and 2, 3, 4, 5, 6, and 7 days post-injury
Result: Significantly reduced cerebral edema, improved motor function, shortened the delay time of sensory neglect, and enhanced spatial learning ability.
Significantly reduced brain tissue damage and weakened the activation of astrocytes and microglia cells.
分子量

483.45

Formula

C22H32NNa2O6P

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
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  • 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.

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产品名称:
EIDD-1723
目录号:
HY-125547
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