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Tirzepatide is a synthetic derivative of gastric inhibitory polypeptide (GIP) that has simultaneous glucagon-like peptide-1 (GLP-1) functionality as well. This combination allows Tirzepatide to lower blood glucose levels, increase insulin sensitivity, boost feelings of satiety, and accelerate weight loss. Tirzepatide was developed to fight type 2 diabetes, but has additionally been shown to protect the cardiovascular system and act as a potent weight loss agent.
| Name | Tirzepatide |
|---|---|
| Sequence | YE-Aib-GTFTSDYSI-Aib-LDKIAQ(C20 fatty acid)AFVQWLIAGGPSSGAPPPS |
| CAS No. | 2023788-19-2 |
| Purity | 99% |
| Appearance | Lyophilized Powder |
| Molecular Formula | C225H348N46O68 |
| Molecular Weight | 4813.53 g/mol |
| Storage | Store in an air-tight container away from light at 2-8°C. For best preservation, store below -10°C. |
Tirzepatide is an analog of the human GIP hormone with a C20 fatty-diacid portion attached, used to optimize the uptake and metabolism of the compound. The fatty-diacid section (eicosanedioic acid) is linked via a glutamic acid and two (2-(2-aminoethoxy)ethoxy)acetic acid units to the side chain of the lysine residue. This arrangement allows for a much longer half-life, extending the time between doses, because of its high affinity to albumin.
Tirzepatide has a greater affinity to GIP receptors than to GLP-1 receptors, and this dual agonist behavior has been shown to produce greater reductions of hyperglycemia compared to a selective GLP-1 receptor agonist. Signaling studies reported that tirzepatide mimics the actions of natural GIP at the GIP receptor. At the GLP-1 receptor, though, tirzepatide shows bias towards cAMP (a messenger associated with regulation of glycogen, sugar, and lipid metabolism) generation, rather than β-arrestin recruitment. This combination of preference towards GIP receptor and distinct signaling properties at GLP-1 suggest this biased agonism increases insulin secretion.
Tirzepatide has been reported to increase levels of adiponectin, an adipokine involved in the regulation of both glucose and lipid metabolism, with a maximum increase of 26% from baseline after 26 weeks, at the 10 mg dosage.
Source from Wikipedia
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