Semaglutide TFA

SKU: orb1708552

Description

Semaglutide TFA is a GLP-1 receptor agonist used in research for type 2 diabetes and obesity. It promotes weight loss, improves glycemic control, and reduces cardiovascular risk, with transient GI effects as common side effects. This analog is applicable in both in vitro binding assays and in vivo metabolic disease models.

Research Area

Immunology & Inflammation; Pharmacology & Drug Discovery, Pharmacology & Drug Discovery

Key Properties

• MW: 4225.6482
• Purity: 99.69% (May vary between batches)
• Formula: C₁₈₉H₂₉₀F₃N₄₅O₆₁
• SMILES: CC[C@@H]([C@@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(NCC(O)=O)=O)CCCNC(N)=N)=O)=O)CCCNC(N)=N)=O)C(C)C)=O)CC(C)C)=O)Cc(cn1)c2c1cccc2)=O)C)=O)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](C(C)C)NC([C@@H](NC([C@@H](NC([C@H]([C@H](O)C)NC([C@@H](NC([C@H]([C@H](O)C)NC(CNC([C@@H](NC(C(C)(NC([C@H](Cc3ncnc3)N)=O)C)=O)CCC(O)=O)=O)=O)=O)Cc4ccccc4)=O)=O)CO)=O)CC(O)=O)=O)=O)CO)=O)CO)=O)Cc5ccc(O)cc5)=O)CC(C)C)=O)CCC(O)=O)=O)=O)CCC(N)=O)=O)C)=O)C)=O)CCCCNC(COCCOCCNC(COCCOCCNC(CC[C@H](C(O)=O)NC(CCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)=O)CCC(O)=O)=O)Cc6ccccc6)=O)C.OC(C(F)(F)F)=O
• Target: Glucagon Receptor
• Solubility: DMSO:80 mg/mL (18.93 mM);H2O:80 mg/mL (18.93 mM)

Bioactivity

• Target IC50:
  GLP1 receptor:0.38 nM (Kd)
• In Vivo:
  The plasma half-life of Semaglutide TFA was 46 hours after intravenous injection and the mean retention time (MRT) was 63.6 hours after subcutaneous injection in a small pig study. Semaglutide TFA significantly ameliorated dyskinesia induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). In addition, it protects dopaminergic neurons in the brain by restoring tyrosine hydroxylase (TH) levels, attenuating inflammatory responses, reducing lipid peroxidation, inhibiting apoptosis and promoting the expression of autophagy-related proteins. Semaglutide TFA shows better results in most aspects compared to liraglutide. Semaglutide TFA lowers blood glucose by promoting insulin secretion and is also effective in reducing body weight.
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• In Vitro:
  Semaglutide TFA is a modified GLP-1 analog with two substitutions (Aib and Arg) at amino acids 8 and 34 and a chemical modification of the lysine at position 26 compared to human GLP-1. It has an affinity for the GLP-1 receptor of 0.38 nM. The amino acid sequence of Semaglutide TFA shares 94% homology with human GLP-1.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

910463-68-2, 910463-68-2 free base, GLP-1 receptor, GlucagonReceptor, Glucagon Receptor, Semaglutide TFA, Semaglutide TFA (910463 68 2 free base), Semaglutide TFA (910463682 free base), Semaglutide TFA (910463-68-2 free base)

Quick Database Links

Gene Symbol

Glucagon Receptor