SBC-115076
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522510

CAS#: 489415-96-5

Description: SBC-115076 is a potent extracellular proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist.


Chemical Structure

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SBC-115076
CAS# 489415-96-5

Theoretical Analysis

MedKoo Cat#: 522510
Name: SBC-115076
CAS#: 489415-96-5
Chemical Formula: C31H33N3O5
Exact Mass: 527.24
Molecular Weight: 527.620
Elemental Analysis: C, 70.57; H, 6.30; N, 7.96; O, 15.16

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 650 Ready to ship
200mg USD 950 Ready to ship
500mg USD 1650 Ready to ship
1g USD 2650 Ready to ship
2g USD 3650 2 weeks
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Synonym: SBC-115076; SBC 115076; SBC115076.

IUPAC/Chemical Name: 4-(4-(benzyloxy)-3-methylbenzoyl)-3-hydroxy-1-(3-morpholinopropyl)-5-(pyridin-4-yl)-1H-pyrrol-2(5H)-one

InChi Key: UNINQWCCZAGYSH-UHFFFAOYSA-N

InChi Code: 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/h2-4,6-13,20,28,36H,5,14-19,21H2,1H3

SMILES Code: O=C1N(CCCN2CCOCC2)C(C3=CC=NC=C3)C(C(C4=CC=C(OCC5=CC=CC=C5)C(C)=C4)=O)=C1O

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

More Info:

Biological target: SBC-115076 is a potent proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor.
In vitro activity: SBC-115076 demonstrated potential in preventing atherosclerosis accelerated by homocysteine (Hcy) in vitro. SBC-115076inhibited PCSK9, reducing lipid accumulation and restoring cholesterol efflux via ABCA1 and ABCG1 in THP-1 macrophages exposed to Hcy. Reference: Front Cardiovasc Med. 2021 Oct 1;8:746989. https://pubmed.ncbi.nlm.nih.gov/34660746/
In vivo activity: In rats fed a high-fat diet (HFD), treatment with SBC-115076 and atorvastatin resulted in reduced body weight, visceral fat, and cholesterol levels compared to vehicle-treated rats. However, SBC-115076 showed greater efficacy in mitigating obesity and dyslipidemia than the high-dose atorvastatin, indicating a more substantial effect in countering the effects of the high-fat diet. Notably, the levels of HDL cholesterol did not exhibit differences among the groups. Reference: Toxicol Appl Pharmacol. 2019 Nov 1;382:114741. https://pubmed.ncbi.nlm.nih.gov/31473249/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.0 87.18
DMSO:PBS (pH 7.2) (1:1) 0.5 0.95
DMF 2.0 3.79

Preparing Stock Solutions

The following data is based on the product molecular weight 527.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Jin P, Gao D, Cong G, Yan R, Jia S. Role of PCSK9 in Homocysteine-Accelerated Lipid Accumulation in Macrophages and Atherosclerosis in ApoE-/- Mice. Front Cardiovasc Med. 2021 Oct 1;8:746989. doi: 10.3389/fcvm.2021.746989. PMID: 34660746; PMCID: PMC8517151. 2. Wu C, Lin D, Ji J, Jiang Y, Jiang F, Wang Y. PCSK9 Inhibition Regulates Infarction-Induced Cardiac Myofibroblast Transdifferentiation via Notch1 Signaling. Cell Biochem Biophys. 2023 Jun;81(2):359-369. doi: 10.1007/s12013-023-01136-1. Epub 2023 Apr 21. PMID: 37081375. 3. Thonusin C, Apaijai N, Jaiwongkam T, Kerdphoo S, Arunsak B, Amput P, Palee S, Pratchayasakul W, Chattipakorn N, Chattipakorn SC. 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. doi: 10.1016/j.taap.2019.114741. Epub 2019 Aug 29. PMID: 31473249.
In vitro protocol: 1. Jin P, Gao D, Cong G, Yan R, Jia S. Role of PCSK9 in Homocysteine-Accelerated Lipid Accumulation in Macrophages and Atherosclerosis in ApoE-/- Mice. Front Cardiovasc Med. 2021 Oct 1;8:746989. doi: 10.3389/fcvm.2021.746989. PMID: 34660746; PMCID: PMC8517151.
In vivo protocol: 1. Wu C, Lin D, Ji J, Jiang Y, Jiang F, Wang Y. PCSK9 Inhibition Regulates Infarction-Induced Cardiac Myofibroblast Transdifferentiation via Notch1 Signaling. Cell Biochem Biophys. 2023 Jun;81(2):359-369. doi: 10.1007/s12013-023-01136-1. Epub 2023 Apr 21. PMID: 37081375. 2. Thonusin C, Apaijai N, Jaiwongkam T, Kerdphoo S, Arunsak B, Amput P, Palee S, Pratchayasakul W, Chattipakorn N, Chattipakorn SC. 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. doi: 10.1016/j.taap.2019.114741. Epub 2019 Aug 29. PMID: 31473249.

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