Tirzepatide
Tirzepatide is a first-in-class, long-acting dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. It is a 39-amino-acid modified synthetic peptide conjugated with a C20 fatty diacid moiety, which enables albumin binding to prolong its half-life and extend pharmacodynamic activity for once-weekly dosing in metabolic disease research and clinical use.
Tirzepatide is a first-in-class, long-acting dual agonist of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors, a 39-amino-acid modified synthetic peptide with albumin-binding C20 fatty diacid conjugation to extend circulating half-life for once-weekly administration:
Core Mechanism & Key Properties
- Selectively activates both GIP and GLP-1 receptors, delivering complementary metabolic effects:
- GLP-1 receptor activation: glucose-dependent insulin secretion, glucagon suppression, delayed gastric emptying, reduced appetite, and weight loss
- GIP receptor activation: enhanced insulin sensitivity, improved lipid metabolism, and amplified weight loss efficacy beyond single-target GLP-1 agonists
- Albumin-binding conjugation extends circulating half-life to ~5 days, enabling once-weekly dosing
- FDA-approved for three clinical indications: type 2 diabetes glycemic control, chronic weight management (obesity/overweight with comorbidities), and obstructive sleep apnea in obese patients
- Superior glycemic control and weight loss efficacy compared to single-target GLP-1 receptor agonists in Phase 3 clinical trials
Primary Research Applications
- Type 2 diabetes and glycemic regulation research
- Obesity and metabolic syndrome weight management studies
- Non-alcoholic steatohepatitis (MASH) and cardiovascular disease preclinical and clinical investigations
- Heart failure with preserved ejection fraction (HFpEF) therapeutic research
- Dual incretin receptor signaling mechanism studies
Manufactured to ≥98% purity, sterile-filtered, and lyophilized for long-term stability.
For laboratory research use only; not intended for human or veterinary administration outside of approved clinical protocols.
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