• Tirzepatide (LY3298176), 99% purity peptide (TFA removed)

Tirzepatide (LY3298176), 99% purity peptide (TFA removed)

Not For Human Use, Lab Use Only.

Cat.#: 318942

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Product Information

  • Product Name
    Tirzepatide (LY3298176), 99% purity peptide (TFA removed)
  • Documents
  • Sequence
    YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS (X2 and X13 are α-amino isobutyric acid (Aib), S39 is L-serinamide, and K20 is N6-{N-(hydrogen icosanedioyl)-γ-Glu-bis[iminobis(ethylenoxy)acetyl]}-Lysine)
  • Three letter code
    Tyr-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{N6-{N-(hydrogen icosanedioyl)-γ-Glu-bis[iminobis(ethylenoxy)acetyl]}-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser- Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
  • Length (aa)
    39
  • Peptide Purity (HPLC)
    99.38%
  • Molecular Formula
    C225H348N48O68
  • Molecular Weight
    4813.45
  • Source
    Synthetic
  • Additional Information
    The Net Peptide Content (NPC) of current batch (MTFA30421-0830) is 91.17%.

    Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis. Early phase trials in T2DM indicate that tirzepatide improves clinical outcomes beyond those achieved by a selective GLP-1 receptor agonist. Tirzepatide was discovered by engineering GLP-1 activity into the GIP sequence. It is an imbalanced dual agonist in favor of GIPR over GLP-1R activity as the molecule shows equal affinity for the GIPR compared with native GIP but binds the GLP-1R with approximately 5-fold weaker affinity than native GLP-1. The imbalanced nature of tirzepatide may be critical to maximizing the efficacy of a dual agonist because dose escalation for GLP-1R activation can be limited by gastrointestinal effects such as nausea and vomiting, while GIPR engagement is not known to be associated with similar events. As a consequence, a pharmacological profile favoring potency at the GIPR offers an opportunity to fully engage this pathway while minimizing GLP-1–related tolerability issues. In addition to a potency ratio toward GIPR activity, tirzepatide contains a C20 unsaturated di-acid acyl chain to affect albumin binding, and the overall properties of the molecule enable once-weekly dosing. Beyond convenience, this pharmacokinetic feature may confer pharmacodynamic benefit, as high and sustained concentrations of selective GLP-1R agonists have enhanced clinical efficacy.

    Notes:

    • *Tirzepatide (LY3298176) is lyophilized in a package of 5mg/tube.
    • Store lyophilized Tirzepatide (LY3298176) in a refrigerator at -20°C to 4°C (-4°F to 39°F)
    • If needed, liquid Tirzepatide (LY3298176) can be stored unrefrigerated at temperatures not to exceed 30ºC (86ºF) for up to 3 weeks.
    • Do not freeze liquid Tirzepatide (LY3298176).
    • Store Tirzepatide (LY3298176) in the original tube and protect it from light.
    • This product is not sterile, please sterilize it by filtration before cell assays or animal experiments.
  • Storage Guidelines
    Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual:Handling and Storage of Synthetic Peptides
  • References
    • Willard FS, Douros JD, Gabe MB, Showalter AD, Wainscott DB, Suter TM, et al. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight. 2020;5(17)
    • Min T, Bain SC. The Role of Tirzepatide, Dual GIP and GLP-1 Receptor Agonist, in the Management of Type 2 Diabetes: The SURPASS Clinical Trials. Diabetes Ther. 2021;12(1):143-157
    • Willard FS, Douros JD, Gabe MB, Showalter AD, Wainscott DB, Suter TM, et al. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight. 2020;5(17)
  • About TFA salt

    Trifluoroacetic acid (TFA) is a strong acid, which is commonly used to cleave synthesized peptides from solid-phase resins and is also used to improve HPLC performance in the peptide purification step. By default, custom peptides are delivered as lyophilized TFA salts, and can contain as much as 10-45% TFA.

    TFA in custom peptides can cause inexplicable discrepancies in subsequent assay data. For instance, TFA in nM concentrations has been shown to interfere with cellular assays, inhibiting cellular proliferation in some instances, and increasing cell viability in others . It has also been found to be an unintended allosteric modulator of the glycine receptor, GlyR.

    TFA Removal Service is recommended for:

    • Peptides that will be used in cellular assays
    • Peptides that will be used as APIs or in manufactured products
    • For hydrophilic peptides containing numerous basic residues

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Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE"