SBC-115076
目录号 : GC17417
An inhibitor of PCSK9 action
Cas No.:489415-96-5
Sample solution is provided at 25 µL, 10mM.
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PCSK9 is a serine protease mainly expressed in the liver and the intestine. It acts by reducing the amount of LDLR in hepatocytes. PCSK9 enzymatic activity permits its intracellular maturation, followed by secretion. Circulating PCSK9 binds the LDLR on the cell surface and is subsequently cointernalized together with the LDLR. PCSK9 can also bind the LDLR intracellularly. Thus, by virtue of its role as a major inhibitor of the LDLR, PCSK9 has emerged as a hot new drug target to treat hypercholesterolemia and coronary heart disease. SBC-115076 is an anti-PCSK9 compound.
In vitro: It was found that SBC-115076 could dose-dependently increase the DHLDL uptake, which was lower than that SBC-110034 did. Moreover, SBC-115076 could increase several folds of the intracellular LDLR level at 1.6 μM [1].
In vivo: SBC-115076 was observed to lower cholesterol levels in mice that were fed high fat diet. Results showed data obtained with SBC-115076 indicating a mean of 32% reduction in total cholesterol levels after two weeks relative to high fat diet animal levels and a mean 50% reduction toward return to regular diet cholesterol levels [1].
Clinical trial: Up to now, SBC-115076 is still in the preclinical development stage.
Reference:
[1] Anti-proprotein convertase subtilisin kexin type 9 (anti-pcsk9) compounds and methods of using the same in the treatment and/or prevention of cardiovascular diseases. Patent: WO 2014150326 A1
| Cas No. | 489415-96-5 | SDF | |
| 化学名 | 4-(4-(benzyloxy)-3-methylbenzoyl)-3-hydroxy-1-(3-morpholinopropyl)-5-(pyridin-4-yl)-1H-pyrrol-2(5H)-one | ||
| Canonical SMILES | CC1=CC(C(C(C(N2CCCN3CCOCC3)C4=CC=NC=C4)=C(O)C2=O)=O)=CC=C1OCC5=CC=CC=C5 | ||
| 分子式 | C31H33N3O5 | 分子量 | 527.61 |
| 溶解度 | ≥ 52.8mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8953 mL | 9.4767 mL | 18.9534 mL |
| 5 mM | 0.3791 mL | 1.8953 mL | 3.7907 mL |
| 10 mM | 0.1895 mL | 0.9477 mL | 1.8953 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet