Tirzepatide (LY3298176) – Dual GIP/GLP-1 Receptor Agonist – ≥98% Purity Lyophilized Powder – For Research Use Only

Tirzepatide (LY3298176) – Dual GIP/GLP-1 Receptor Agonist – High Purity Lyophilized Powder – For Research Use Only

 

High-purity Tirzepatide (LY3298176), a first-in-class dual GIP/GLP-1 receptor agonist. ≥98% purity by HPLC. CAS 2023788-19-2. Molecular weight 4,813.45 Da. Lyophilized powder for research applications including metabolic studies, incretin receptor pharmacology, and obesity/T2D model research. Bulk wholesale available with COA and global shipping.

 

Tirzepatide (LY3298176) is a first-in-class, once-weekly dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist . It represents a significant advance in incretin-based therapies, being the first commercially approved molecule to successfully combine agonism at both major incretin receptors in a single peptide .

The molecule is a 39-amino acid linear peptide conjugated to a C20 fatty di-acyl moiety via a hydrophilic linker at a lysine residue in the middle of the molecule, which extends its half-life for once-weekly dosing .

Scientific Background

Tirzepatide functions through a unique imbalanced and biased agonism profile at the two receptors :

This biased agonism at the GLP-1R (preferential cAMP signaling over β-arrestin recruitment) results in prolonged receptor activity, reduced desensitization, and potentially improved tolerability compared to full GLP-1R agonists .

Key Therapeutic Indications (Clinical Context)

Tirzepatide has received regulatory approvals worldwide:

Additional approvals have been granted in the EU, Japan, and China (May 2024) . Global sales reached **$5.163billionin2023\ast \ast and$2.324 billion in Q1 2024 alone .

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Key Features

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Mechanism of Action (Research Context)

Tirzepatide is a dual agonist at two key incretin receptors involved in metabolic regulation :

1. GIP Receptor (GIPR) Activation

GIP is an intestinally derived, insulinotropic hormone that potentiates insulin secretion in response to nutrient intake. Tirzepatide acts as a full agonist at the GIPR, with binding affinity equivalent to native GIP. Unlike selective GLP-1R agonists, the GIPR activation component of tirzepatide contributes to:

• Additional insulin secretion beyond GLP-1R stimulation

• Improved insulin sensitivity independent of weight loss

• Adipose tissue-mediated metabolic effects

Research Debate (Agonism vs. Antagonism): Emerging evidence suggests both GIPR agonism (tirzepatide) and GIPR antagonism (MariTide/AMG-133) produce weight loss in combination with GLP-1R activation, creating a “paradox” in the field . Tirzepatide’s clinical success supports the GIPR agonism approach for obesity and T2D treatment.

2. GLP-1 Receptor (GLP-1R) Activation – Biased Agonism

Tirzepatide binds to GLP-1R with approximately 5-fold lower affinity than native GLP-1. However, it demonstrates biased agonism – preferential activation of cAMP signaling over β-arrestin recruitment :

This biased profile means that in cells with high GLP-1R density (e.g., pancreatic β-cells), tirzepatide generates a full cAMP response. In lower density tissues (e.g., CNS), reduced desensitization allows prolonged physiological effect .

Therapeutic Advantages of Biased Agonism

The reduction in β-arrestin recruitment at the GLP-1R may translate to:

• Prolonged insulin secretion – less receptor desensitization

• Potential for reduced nausea – a rate-limiting factor in GLP-1R agonist dose escalation

• Sustained efficacy – once-weekly dosing despite lower receptor affinity

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Research Applications

Comparative Efficacy Note: Clinical studies demonstrate that tirzepatide produces greater HbA1c reduction and weight loss compared to semaglutide, with the lowest dose of tirzepatide outperforming 1 mg weekly semaglutide for glycemic control .

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Specifications – Bulk/Wholesale Format

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Reconstitution Instructions (For Research Use Only)

For a 60 mg vial (reference standard):

1. Reconstitute with 4 mL sterile water to achieve a concentration of 15 mg/mL

2. Gently swirl – do not shake vigorously

3. Store reconstituted solution at 2-8°C and use within 90 days

4. For smaller vials, adjust volume proportionally

General Reconstitution Protocol:

• For in vivo research: Reconstitute in sterile saline or PBS

• For in vitro research: Reconstitute in appropriate buffer (5% acetic acid may aid solubility)

• Aliquot immediately after reconstitution to avoid repeated freeze-thaw cycles

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Regulatory Status & Manufacturing Quality

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Comparison: Tirzepatide vs. Selective GLP-1R Agonists

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Compliance & Disclaimer

⚠️ FOR RESEARCH USE ONLY. NOT FOR HUMAN OR VETERINARY USE.

This product is sold for laboratory research purposes only. It is not a pharmaceutical, drug, or medical device. Not intended for diagnostic, therapeutic, or in vivo human applications. Not for use in food, cosmetics, or household products.

Tirzepatide is the active ingredient in FDA-approved commercial drugs Mounjaro® and Zepbound®. This product is not for human administration. Any use in competitive animals or humans is strictly prohibited.

By purchasing this product, you affirm that you are a qualified research professional and that you will use this product only in lawful, ethical research applications.

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Why Source From Us?

• ✅ High-purity peptides (≥98% to ≥99% by HPLC)

• ✅ GMP-certified manufacturing facilities (ISO9001, cGMP)

• ✅ US-DMF filed (DMF 040115) – simplifies regulatory compliance for customers

• ✅ Kilogram-scale production capability – stable, continuous batches

• ✅ Third-party COA (Certificate of Analysis) available for each batch

• ✅ OEM/ODM services available (custom purity, vial size, labeling)

• ✅ Bulk wholesale pricing – significant discounts for large-volume orders

• ✅ Discreet worldwide shipping via DHL, FedEx, UPS

• ✅ Free samples available for qualified research institutions

• ✅ Refund/replacement policy for quality issues

Contact us for wholesale pricing, COA requests, bulk quotations, regulatory documentation (DMF reference letter), and shipping details. Long‑term research supply partnerships welcome.

 

 

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