BL-918|cas:2101517-69-3|西域试剂

BL-918,99.98%

产品编号：Bellancom-124729| CAS NO：2101517-69-3| 分子式：C₂₃H₁₅F₈N₃OS| 分子量：533.44

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货号	价格	库存与货期
Bellancom-124729	￥1550.00	杭州北京（现货）
Bellancom-124729	￥2350.00	杭州北京（现货）
Bellancom-124729	￥6950.00	杭州北京（现货）
Bellancom-124729	￥12000.00	杭州北京（现货）

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BL-918

产品介绍

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。

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.

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

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
(In Vivo)

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).

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

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.

体内研究

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

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.

体内研究

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

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.

性状

Solid

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。