1. Apoptosis Cell Cycle/DNA Damage Autophagy Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel
  2. FKBP Calcium Channel
  3. ILS-920

ILS-920 是一种非免疫抑制性雷帕霉素类似物,具有有效的神经保护活性。ILS-920 选择性结合亲免蛋白 FKBP52 和 L 型电压门控钙通道 (VGCC) 的 β1 亚基。ILS-920 对 FKBP52 的选择性是 FKBP12 的 200 倍。ILS-920 可大大降低了免疫抑制活性。

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ILS-920 Chemical Structure

ILS-920 Chemical Structure

CAS No. : 892494-07-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12[1].

IC50 & Target

L-type calcium channel

 

体外研究
(In Vitro)

ILS-920 promotes neuronal survival and stimulates neurite outgrowth with potent neurotrophic activities in cortical neuronal cultures[1].
ILS-920 can inhibit L-type Ca2+ channels in rat hippocampal neurons and F-11 dorsal root ganglia (DRG)/neuroblastoma cells. ILS-920 can protect neurons from Ca2+-induced cell death by modulating Ca2+ channels and promote neurite outgrowth via FKBP52 binding[1].

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

体内研究
(In Vivo)

In a transient middle cerebral artery occlusion (tMCAO) model of ischemic stroke, ILS-920, administered 4 h postocclusion at 10 and 30 mg/kg, significantly reduces infarct volume by 24% and 23% in 72 h, respectively, and robustly enhances functional recovery measured by improvement in neurological deficits[1].

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

Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT00827190Wyeth is now a wholly owned subsidiary of Pfizer
Acute Ischemic Stroke
February 2009Phase 1
分子量

1023.30

Formula

C57H86N2O14

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
  • 摩尔计算器

  • 稀释计算器

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质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
ILS-920
目录号:
HY-106345
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