Semaglutide Glucagon Receptor for The Treatment Of Diabetes

English name：Semaglutide

CAS number：910463-68-2

Molecular formula: C187H291N45O59

Molecular weight: 4113.57754

EINECS number: 203-405-2

Related category

Polypeptides - customer peptides; Pharmaceutical raw materials; Biopharmaceutical; Ingredients; Inhibitor; Biochemical reagent - protein; Drug polypeptide; Peptides; Polypeptide intermediate; Organic intermediates; GLPChemicalbook; PP; APIs; API; Polypeptide; Polypeptide apis; Drug peptide; Chemical Industry; Reagent for scientific research; Raw materials; Biological reagent; Chemicals; Chemical products; Chemical reagent; Daily raw materials

Mol file：910463-68-2.mol

Structural formula:

Properties of sommarlutide

Storage: Store at -20°C

Solubility: dimethyl sulfoxide: 3mg/mL (0.73mM)

Form: solid

Color: White to beige

InChIKey：DLSWIYLPEUIQAV-CCUURXOWSA-N

Intro

semaglutide is a new generation GLP-1 (glucagon-like peptide-1) analogue developed by NovoNordisk, Denmark. Semaglutide is a long-acting formulation based on the basic structure of Liraglutide, which is more effective in treating type 2 diabetes. Novo Nordisk has completed six ChemicalbookPhaseIIIa studies for its once-weekly injection of Sommarlutide and submitted a new drug registration application to the U.S. Food and Drug Administration (FDA) on December 5, 2016. An application for Marketing Authorization (MAA) has also been submitted to the European Medicines Agency (EMA). On the other hand, a once-daily oral formulation of sommarlutide is currently in phase III.

Effect

Sommarlutide is a long-acting formulation based on the basic structure of Liraglutide, which is more effective in the treatment of type 2 diabetes.

Preparation

Sommarutide was prepared by solid-liquid phase synthesis method. Straight chain peptide Aib8, Arg34GLP-1(7-37) and fatty side chain acylating agent were prepared by solid phase synthesis method, and the straight chain peptide Lys26 was modified by the fatty chain acylating agent synthesized by Chemicalbook under alkaline conditions to obtain sommarutide. The bioactivity of the self-made samples was determined by time-resolved fluorescence resonance energy transfer immunoassay.

New drug class of GLP-1 receptor agonists

Semeglutide is a novel GLP-1 analogue that is injected subcutaneously once a week. Sommarlutide is a long-acting GLP-1 analogue developed by Novo Nordisk with 1 /w subcutaneous injection. Compared with lilaplutide, sommarlutide has a longer fat chain and an increased hydrophobicity, but sommarlutide is modified by short chain PEG and its hydrophilicity is greatly enhanced. After PEG modification, Chemicalbook not only binds closely to albumin, conceals the hydrolysis site of DPP-4 enzyme, but also reduces renal excretion, prolongs biological half-life, and achieves the effect of long cycle. Novo Nordisk's sommarutide slings off DPP-4's Sitagliptin, and GLP-1's progenitor, long-acting exenatide (should be designed to compete head-to-head with lilly's trulicity, bullying has long been on the market). In the trial, high dose of soma decreased A1C1.6% and reduced body weight up to 6kg.

The trial examined the efficacy and safety of 1.0 mg of sommarutide versus a weekly injection of 2.0 mg of exenatide in 813 patients with type 2 diabetes over a period of 56 weeks, with oral administration of one or two antidiabetic drugs.

In December 2017, the FDA officially approved NovoNordisk's once-a-week GLP-1 drug, Sommarutide, under the brand name Ozempic. According to clinical trial data, Ozempic reduced HbA1c levels compared with Chemicalbook placebo, Merck's Januvia, Astrazeneca's Bydureon and Sanofi's Lantus. The drug has also shown an ability to help patients lose weight.

As a leader in the field of diabetes, NovoNordisk (NovoNordisk) not only in the field of insulin three points, its development of human glucagon like peptide-1 (GLP-1) analog Liraglutide (LirChemicalbookaglutide), trade name: Victoza, since its listing in 2009, has dominated the GLP-1 market, with global sales of up to $3.2 billion in 2016.

Liraglutide has expired, and generic drug companies are eyeing it. To prevent this from happening, Novo Nordisk has already prepared the next generation of Liraglutide, which is sommarlutide. Structurally,Semeglutide is a GLP-1(7-37) chain with 8-bit Aib replacing Ala, 34-bit Arg replacing Lys, and 26-bit Lys attached to octadecanoate fatty chain Chemicalbook. Compared to Liraglutide, Semeglutide has a longer fat chain and an increased hydrophobicity, but Semeglutide is modified by short chain PEG and its hydrophilicity is greatly enhanced. After PEG modification, it can not only bind to albumin closely, cover the hydrolysis site of DPP-4 enzyme, but also reduce renal excretion, prolong biological half-life, and achieve a long cycle effect.

According to the analysis, Ozempic is expected to be one of the best-selling drugs in 2017. Novo Nordisk forecasts drug sales of $2.2 billion in 2022. At the same time, Novo Nordisk is actively developing oral dosage forms of sommarutide, gradually consolidating its dominance in the diabetes field.

Biological activity

Semaglutide (Rybelsus Ozempic, NN9535 OG217SC, NNC0113-0217) is a Chemicalbook long-acting glucagon sample peptide 1 (glp-1) analogue, glp-1 receptor agonist, It has potential therapeutic efficacy for type 2 diabetes mellitus (T2DM).

Target point

Target Value

GLP-1 receptor

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