WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522510
CAS#: 489415-96-5
Description: SBC-115076 is a potent extracellular proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist.
Hodoodo Cat#: H522510
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
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: | TBD |
| In vivo activity: | Body weight, visceral fat, total cholesterol, LDL cholesterol, and triglyceride levels of HFD-fed rats treated with vehicle were signficiantly increased when compared to those of ND-fed rats treated with vehicle. Although both high dose atorvastatin and PCSK9 inhibitor (SBC-115076) significantly reduced body weight, visceral fat and hypercholesterolemia in HFD-fed rats, the PCSK9 inhibitor had a greater efficacy in the attenuation of obesity and dyslipidemia than the high dose atorvastatin (Table 3). Interestingly, HDL cholesterol levels among the four groups did not differ. Reference: Toxicol Appl Pharmacol. 2019 Nov 1;382:114741. https://pubmed.ncbi.nlm.nih.gov/31473249/ |
| 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 |
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. 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: | TBD |
| In vivo protocol: | 1. 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. |
