PCSK9-IN-11
目录号 : GC69671PCSK9-IN-11 (compound 5r) 是一种口服有效的 PCSK9 抑制剂。 PCSK9-IN-11 在 HepG2 细胞中表现出 PCSK9 转录抑制活性,IC50 为 5.7 μM。 PCSK9-IN-11 增加 LDL 受体 (LDLR) 蛋白水平。 PCSK9-IN-11 可用于动脉粥样硬化研究。
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
- Datasheet
IC50: 5.7 μM (PCSK9)[1]
PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research[1].
PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) 以剂量依赖性方式显着降低 PCSK9 蛋白水平并增加 LDLR 表达[1]。
Western Blot Analysis[1]
Cell Line: | HepG2 cells |
Concentration: | 0, 2.5, 5, 12.5, 25 μM |
Incubation Time: | 24 h |
Result: | Significantly decreased PCSK9 protein level in a dose dependent manner. Markedly increased LDLR expression in a dose dependent manner. Significantly and dose-dependently increased DiI-LDL uptake by around 1.7 folds. |
PCSK9-IN-11 (compound 5r) (0-1000 mg/kg,灌胃,once) 具有更好的体内安全特性,半致死剂量 (LD50) 值超过 1000 mg/kg [1]。
PCSK9-IN-11 (30 mg/kg,灌胃,每天一次,持续 8 周) 显著抑制肝脏 PCSK9 表达并略微降低血清 PCSK9 水平[1]。
Animal Model: | C57BL/6J mice[1] |
Dosage: | 0, 250, 500 or 1000 mg/kg |
Administration: | Intragastrically administrated, single dose |
Result: | Exhibited a good in vivo safety feature with the halflethal dose (LD50) value of over 1000 mg/kg. Did not affected the body weight, behavioral and survival characteristics of mice. |
Animal Model: | ApoE KO mice (under high-fat diet (HFD))[1] |
Dosage: | 30 mg/kg |
Administration: | Intragastric administration, once a day for 8 weeks |
Result: | Significantly suppressed hepatic PCSK9 expression and slightly reduced serum PCSK9 level. |
[1]. Qiao MQ, et al. Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis. Eur J Med Chem. 2022 Dec 26;247:115047.
Cas No. | SDF | Download SDF | |
分子式 | C16H17ClFN5O3 | 分子量 | 381.79 |
溶解度 | DMSO : 125 mg/mL (327.41 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6192 mL | 13.0962 mL | 26.1924 mL |
5 mM | 0.5238 mL | 2.6192 mL | 5.2385 mL |
10 mM | 0.2619 mL | 1.3096 mL | 2.6192 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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