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| 25mg |
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Purity: ≥98%
SBC-110736 (SBC110736) is a novel and potent small molecule inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9) with anti-hyperlipidemic effects. It has been reported to be able to lower cholesterol levels in mice. PCSK9 plays a major regulatory role in cholesterol homeostasis, mainly by reducing LDLR levels on the plasma membrane. Several studies have determined the potential use of PCSK9 inhibitors in the treatment of hyperlipoproteinemia (commonly called hypercholesterolemia). Furthermore, loss-of-function mutations in the PCSK9 gene result in lower levels of LDL and protection against cardiovascular disease.
| ln Vivo |
Male C57BL/6 mice, SBC-110736, lower cholesterol in mice given a high-fat diet. Two weeks later, average total cholesterol levels were 38% lower than those of animals fed a high-fat diet, and lower than those of animals fed a high-fat diet. Normal levels of dietary cholesterol are restored by an average reduction of 50% [1].
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| References |
| Molecular Formula |
C26H27N3O2
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|---|---|
| Molecular Weight |
413.5115
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| Exact Mass |
413.21
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| CAS # |
1629166-02-4
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| PubChem CID |
78425817
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
681.1±55.0 °C at 760 mmHg
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| Flash Point |
365.7±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
3.09
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
602
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PILMFSWQYWYOJC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H27N3O2/c1-19-8-14-24(15-9-19)28-16-17-29(25(18-28)21-6-4-3-5-7-21)26(31)22-10-12-23(13-11-22)27-20(2)30/h3-15,25H,16-18H2,1-2H3,(H,27,30)
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| Chemical Name |
N-[4-(2-Phenyl-4-p-tolyl-piperazine-1-carbonyl)-phenyl]-acetamide
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| Synonyms |
SBC110736; SBC 110736; SBC-110736
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~241.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4183 mL | 12.0916 mL | 24.1832 mL | |
| 5 mM | 0.4837 mL | 2.4183 mL | 4.8366 mL | |
| 10 mM | 0.2418 mL | 1.2092 mL | 2.4183 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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