Icerguastat - CAS:951441-04-6

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Icerguastat (Synonyms:Sephin1; IFB-088)

目录号 : KM9741 CAS No. : 951441-04-6 纯度 : 98%

Data Sheet 产品使用指南

Icerguastat (Sephin1) ，一种缺乏 α2-肾上腺素能活性的 Guanabenz 衍生物，是磷酸酶调节亚单位 PPP1R15A (R15A) 的选择性抑制剂。Icerguastat 抑制 eIF2α 去磷酸化，从而延长保护反应。Icerguastat 具有抗朊病毒作用。

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生物活性

Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect.

体外研究

Icerguastat (5 µM) prolongs eIF2α phosphorylation in oligodendrocytes under stress.
Icerguastat (Sephin1) (selective inhibitor of a holophosphatase), safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Sephin1 selectively binds and inhibits the stress-induced PPP1R15A, but not the related and constitutive PPP1R15B, to prolong the benefit of an adaptive phospho-signaling pathway, protecting cells from otherwise lethal protein misfolding stress.

体内研究

Icerguastat (4-8 mg/kg; i.p.; daily for 35 days) delays the onset of EAE (experimental autoimmune encephalomyelitis).
Icerguastat (100 μg; i.p.) prolongs the survival of prion-infected mice.

Animal Model:	C57BL/6J female mice immunized with MOG35-55/CFA to induce chronic EAE
Dosage:	4 mg/kg, 8 mg/kg
Administration:	I.p.; daily for 35 days
Result:	Significantly delayed clinical disease onset with both dosages, but to a greater extent with the 8 mg/kg treatment.

Animal Model:	Five-week-old female FVB mice (intracerebrally with mouse-adapted RML prions)
Dosage:	100 μg
Administration:	I.p.; 3 times per week for 60 days, after 60 days of treatment, the treatment was reduced to two i.p. injections per week for another 20 days.
Result:	Significantly prolonged survival of prion-infected mice.

分子式

C₈H₉N₄Cl

分子量

196.64

CAS号

951441-04-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 50 mg/mL (254.27 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.0854 mL	25.4272 mL	50.8544 mL
5 mM	1.0171 mL	5.0854 mL	10.1709 mL
10 mM	0.5085 mL	2.5427 mL	5.0854 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (10.58 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (10.58 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (10.58 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (10.58 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

临床试验

纯度： 98%

Data Sheet

产品使用指南

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