BL-918 - CAS:2101517-69-3

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BL-918

目录号 : KM3027 CAS No. : 2101517-69-3 纯度 : 98%

Data Sheet 产品使用指南

BL-918 是一种具有口服活性 UNC-51 样激酶 1 (ULK1) 激活剂，EC₅₀ 为 24.14 nM。BL-918 通过靶向 ULK 复合物发挥其细胞保护性自噬作用。BL-918 有用于帕金森氏病 (PD) 的潜力。

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10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC₅₀ of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.

体外研究

BL-918 (compound 33i) binds to ULK1 with a high binding affinity (K_D=0.719 μM).
BL-918 (5 μM; for 24 hours) induces autophagy in Neuron-Like SH-SY5Y cells.
BL-918 (0.5-50 μM; for 24 hours) can partially reverse MPP-induced cell death, which is determined by enhancing cell viability.
BL-918 (5 μM; for 6-36 hours) time-dependently elevates the expression levels of LC3-II, Beclin-1, and its phosphorylation status, whereas reduces the level of the selective autophagy substrate SQSTM1/p62. BL-918 elevates Ser317 and Ser555 phosphorylation of ULK1, as well as decreases Ser757 phosphorylation of ULK1.

Cell Autophagy Assay

Cell Line:	SH-SY5Y cells
Concentration:	5 μM
Incubation Time:	For 24 hours
Result:	Induced Autophagy.

Cell Viability Assay

Cell Line:	SH-SY5Y cells
Concentration:	0.5, 5, 50 μM
Incubation Time:	For 24 hours
Result:	Could partially reverse MPP-induced cell death, which was determined by enhancing cell viability.

Western Blot Analysis

Cell Line:	SH-SY5Y cells
Concentration:	5 μM
Incubation Time:	6, 12, 24, 36 hours
Result:	Time-dependently elevated the expression levels of LC3-II (a key marker of autophagy), Beclin-1, and its phosphorylation status, whereas reduced the level of the selective autophagy substrate SQSTM1/p62.

体内研究

BL-918 (compound 33i; 20, 40, or 80 mg/kg/day; oral gavage; began 2 days before the first injection of saline/MPTP and continuously maintained for 5 days after the last injection of saline/MPTP) attenuates the loss of DA and its metabolites. BL-918 obviously decreases the levels of dopamine (DA), 3,4-dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA).

Animal Model:	Male C57BL/6 mice (eight-week old) weighing between 20 and 25 g
Dosage:	20, 40, or 80 mg/kg
Administration:	Oral gavage; daily; began 2 days before the first injection of saline/MPTP and continuously maintained for 5 days after the last injection of saline/MPTP
Result:	Attenuated the loss of DA and its metabolites.

分子式

C₂₃H₁₅F₈N₃Os

分子量

533.44

CAS号

2101517-69-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 250 mg/mL (468.66 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8746 mL	9.3731 mL	18.7463 mL
5 mM	0.3749 mL	1.8746 mL	3.7492 mL
10 mM	0.1875 mL	0.9373 mL	1.8746 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。-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 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.90 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.90 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。