Tirzepatide
[CAS# 2023788-19-2]

Identification

• Classification: API >> Other chemicals
• Name: Tirzepatide
• Synonyms: LY 3298176; LY3298176; 20-[[4-[2-[2-[2-[2-[2-[2-[[5-[[5-amino-2-[2-[[2-[[6-amino-2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-2-methylpropanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]propanoylamino]-5-oxopentanoyl]amino]-6-[[1-[[1-[[1-[[5-amino-1-[[1-[[1-[[1-[[1-[[2-[[2-[2-[[1-[[1-[[2-[[1-[2-[2-[2-[(1-amino-3-hydroxy-1-oxopropan-2-yl)carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-20-oxoicosanoic acid
• Molecular Formula: C₂₂₅H₃₄₈N₄₈O₆₈
• Molecular Weight: 4813.45
• Protein Sequence: YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS
• CAS Registry Number: 2023788-19-2
• EC Number: 889-790-3
• SMILES: CC[C@H](C)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](C(=O)O)NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC2=CNC3=CC=CC=C32)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N4CCC[C@H]4C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N5CCC[C@H]5C(=O)N6CCC[C@H]6C(=O)N7CCC[C@H]7C(=O)N[C@@H](CO)C(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)C(C)(C)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](CC8=CC=C(C=C8)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC9=CC=CC=C9)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@H](CC1=CC=C(C=C1)O)N

Properties

• Solubility: <1 mg/mL (water)

Safety Data

• Hazard Symbols: GHS08 Warning
• Risk Statements: H361d
• Safety Statements: P203-P280-P318-P405-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Reproductive toxicity	Repr.	2	H361d

Discovery and Applications

Tirzepatide is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist developed by Eli Lilly and Company. It emerged from extensive research into incretin hormones, which are crucial in regulating glucose metabolism. The innovative approach of combining GIP and GLP-1 receptor agonism aimed to enhance the therapeutic effects on blood glucose regulation and weight loss. In 2022, Tirzepatide received FDA approval for the treatment of type 2 diabetes, following clinical trials that demonstrated its superior efficacy in lowering blood sugar levels and promoting weight loss compared to other treatments.

Tirzepatide is used to improve glycemic control in adults with type 2 diabetes. By activating both GIP and GLP-1 receptors, it enhances insulin secretion, inhibits glucagon release, and slows gastric emptying. These combined actions lead to significant reductions in blood glucose levels. Clinical trials have shown that Tirzepatide is more effective in lowering HbA1c, a key marker of long-term blood glucose control, than existing GLP-1 receptor agonists.

Beyond its glucose-lowering effects, Tirzepatide has shown remarkable efficacy in promoting weight loss. It reduces appetite and increases satiety, leading to decreased calorie intake and significant weight reduction. In clinical trials, patients treated with Tirzepatide experienced substantial weight loss

Tirzepatide's impact on weight and glucose metabolism also provides cardiovascular benefits. Obesity and type 2 diabetes are major risk factors for cardiovascular disease, and weight loss combined with improved glycemic control can significantly reduce this risk. The comprehensive benefits of Tirzepatide extend to lowering blood pressure and improving lipid profiles, contributing to better cardiovascular health.

The dual agonist approach of Tirzepatide may extend its benefits to other metabolic disorders, such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH). These conditions are closely linked to obesity and type 2 diabetes, and by addressing the underlying metabolic dysfunctions, Tirzepatide could offer therapeutic benefits.

References

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