SBC-115076 | CAS#489415-96-5 | PCSK9 antagonist

MedKoo Cat#: 522510 | Name: SBC-115076

Description:

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

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

Chemical Structure

SBC-115076

CAS#489415-96-5

Theoretical Analysis

MedKoo Cat#: 522510

Name: SBC-115076

CAS#: 489415-96-5

Chemical Formula: C31H33N3O5

Exact Mass: 527.2420

Molecular Weight: 527.62

Elemental Analysis: C, 70.57; H, 6.30; N, 7.96; O, 15.16

Price and Availability

Size	Price	Availability
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 650.00	Ready to ship
200mg	USD 950.00	Ready to ship
500mg	USD 1,650.00	Ready to ship
1g	USD 2,650.00	Ready to ship
2g	USD 3,650.00	2 weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#C20R07B10

View CoA: current batch, Lot#CRB60222

QC Data

View QC data: current batch, Lot#C20R07B10

View QC data: current batch, Lot#CRB0222

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

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/

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

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

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.

1: Yang Y, Wang Y, Wang Y, Ke T, Zhao L. PCSK9 inhibitor effectively alleviated cognitive dysfunction in a type 2 diabetes mellitus rat model. PeerJ. 2024 Aug 14;12:e17676. doi: 10.7717/peerj.17676. PMID: 39157774; PMCID: PMC11330219. 2: Zhao Y, Liu N, Zhang J, Zhao L. PCSK9i promoting the transformation of AS plaques into a stable plaque by targeting the miR-186-5p/Wipf2 and miR-375-3p/Pdk1/Yap1 in ApoE-/- mice. Front Med (Lausanne). 2024 Feb 26;11:1284199. doi: 10.3389/fmed.2024.1284199. Erratum in: Front Med (Lausanne). 2024 Jun 04;11:1416622. doi: 10.3389/fmed.2024.1416622. PMID: 38596793; PMCID: PMC11002805. 3: Ma Y-X, Chai Y-J, Han Y-Q, Zhao S-B, Yang G-Y, Wang J, Ming S-L, Chu B-B. Pseudorabies virus upregulates low-density lipoprotein receptors to facilitate viral entry. J Virol. 2024 Jan 23;98(1):e0166423. doi: 10.1128/jvi.01664-23. Epub 2023 Dec 6. PMID: 38054618; PMCID: PMC10804996. 4: Cai H, Zheng R, Wu N, Hu J, Wang R, Chi J, Zhang W, Zhao L, Cheng H, Chen A, Li S, Xu L. Chimeric Peptide Engineered Nanomedicine for Synergistic Suppression of Tumor Growth and Therapy-Induced Hyperlipidemia by mTOR and PCSK9 Inhibition. Pharmaceutics. 2023 Sep 23;15(10):2377. doi: 10.3390/pharmaceutics15102377. PMID: 37896137; PMCID: PMC10610039. 5: 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. 6: 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. 7: Thonusin C, Pantiya P, Jaiwongkam T, Kerdphoo S, Arunsak B, Amput P, Palee S, Pratchayasakul W, Chattipakorn N, Chattipakorn SC. A proprotein convertase subtilisin/kexin type 9 inhibitor provides comparable efficacy with lower detriment than statins on mitochondria of oxidative muscle of obese estrogen- deprived rats. Menopause. 2020 Oct;27(10):1155-1166. doi: 10.1097/GME.0000000000001586. PMID: 32576799. 8: 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.