SBC-115076Anti-PCSK9 compound CAS# 489415-96-5 |
Quality Control & MSDS
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| Cas No. | 489415-96-5 | SDF | Download SDF |
| PubChem ID | 5734410 | Appearance | Powder |
| Formula | C31H33N3O5 | M.Wt | 527.61 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 32 mg/mL (60.65 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[hydroxy-(3-methyl-4-phenylmethoxyphenyl)methylidene]-1-(3-morpholin-4-ylpropyl)-5-pyridin-4-ylpyrrolidine-2,3-dione | ||
| SMILES | CC1=C(C=CC(=C1)C(=C2C(N(C(=O)C2=O)CCCN3CCOCC3)C4=CC=NC=C4)O)OCC5=CC=CC=C5 | ||
| Standard InChIKey | VVYIXKBHQQSREP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C31H33N3O5/c1-22-20-25(8-9-26(22)39-21-23-6-3-2-4-7-23)29(35)27-28(24-10-12-32-13-11-24)34(31(37)30(27)36)15-5-14-33-16-18-38-19-17-33/h2-4,6-13,20,28,35H,5,14-19,21H2,1H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | SBC-115076 is an anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compounds, for the treatment and/or prevention of cardiovascular diseases.
Target: PCSK9
in vivo: SBC-115076 lowers cholesterol levels in mice that are fed high fat diet. References: | |||||
SBC-115076 Dilution Calculator
SBC-115076 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8953 mL | 9.4767 mL | 18.9534 mL | 37.9068 mL | 47.3835 mL |
| 5 mM | 0.3791 mL | 1.8953 mL | 3.7907 mL | 7.5814 mL | 9.4767 mL |
| 10 mM | 0.1895 mL | 0.9477 mL | 1.8953 mL | 3.7907 mL | 4.7383 mL |
| 50 mM | 0.0379 mL | 0.1895 mL | 0.3791 mL | 0.7581 mL | 0.9477 mL |
| 100 mM | 0.019 mL | 0.0948 mL | 0.1895 mL | 0.3791 mL | 0.4738 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Description:
IC50: N/A
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
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