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Purity: ≥98%
SBC-115076 (SBC115076) is a potent extracellular proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist, with the potential for the treatment and/or prevention of cardiovascular diseases. SBC-115076 showed a dose-dependent increase of 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. 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
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| ln Vivo |
In high-fat-fed rats, SBC-115076 (4 mg/kg; subcutaneous injection; once daily for 3 weeks) increases insulin sensitivity and decreases adiposity and dyslipidemia [1].
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| Animal Protocol |
Animal/Disease Models: Female Wistar rats (high-fat diet (HFD)- fed)[1]
Doses: 4 mg/kg Route of Administration: Sc; daily for 3 weeks Experimental Results: Superior to atorvastatin in instigating weight loss, cholesterol reduction, and attenuation of Mitochondrial oxidative stress in oxidative muscle fibers of obese female rats. |
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| References |
[1]. Chanisa Thonusin, et al. The comparative effects of high dose atorvastatin and proprotein convertase subtilisin/kexin type 9 inhibitor on the mitochondria of oxidative muscle fibers in obese-insulin resistant female rats. Toxicol Appl Pharmacol. 2019 Nov 1;382:114741.
[2]. Wiciński M, et al. PCSK9 signaling pathways and their potential importance in clinical practice. EPMA J. 2017;8(4):391-402. Published 2017 Aug 14. |
| Molecular Formula |
C31H33N3O5
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| Molecular Weight |
527.61
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| CAS # |
489415-96-5
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| Related CAS # |
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| SMILES |
O1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C([H])([H])C([H])([H])C([H])([H])N1C(C(/C(=C(/C2C([H])=C([H])C(=C(C([H])([H])[H])C=2[H])OC([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])\O[H])/[C@]1([H])C1C([H])=C([H])N=C([H])C=1[H])=O)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.74 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 (4.74 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 (4.74 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 | 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 |
*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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