Tirzepatide (CAS 2023788-19-2) – High‑Purity GIP/GLP‑1 Dual Receptor Agonist API

1. Product Overview

1.1 Product Description

Tirzepatide is a synthetic 39‑amino acid peptide that acts as a dual glucose‑dependent insulinotropic polypeptide (GIP) receptor and glucagon‑like peptide‑1 (GLP‑1) receptor agonist. It is the first molecule of its class approved for the treatment of type 2 diabetes mellitus and chronic weight management. As an active pharmaceutical ingredient (API), tirzepatide is supplied as a lyophilized powder or solution for subcutaneous injection after reconstitution.

The molecule contains two non‑natural amino acid residues (Aib, α‑aminoisobutyric acid) that improve proteolytic stability and plasma half‑life. A C‑terminal amide and a side‑chain fatty diacid (C20) enable albumin binding, prolonging the action to once‑weekly dosing.

1.2 Key Specifications at a Glance

  • CAS Number: 2023788-19-2

  • Molecular Formula: C₂₂₅H₃₄₈N₄₈O₆₈

  • Molecular Weight: 4,813.5 g/mol (peptide portion)

  • Purity (by HPLC): ≥98.0% (research grade); ≥99.0% (pharmaceutical grade)

  • Appearance: White to off‑white lyophilized powder or amorphous solid

  • Water content (Karl Fischer): ≤8.0%

  • Storage condition: −20 °C, protected from light and repeated freeze‑thaw cycles

2. Chemical & Physical Properties

Property Value
Sequence (single‑letter) YXEGTFTSDYSIXLDKKAQKAFVQWLIAGGPSSGAPPPS
Sequence (three‑letter) H‑Tyr‑Aib‑Glu‑Gly‑Thr‑Phe‑Thr‑Ser‑Asp‑Tyr‑Ser‑Ile‑Aib‑Leu‑Asp‑Lys‑Lys‑Ala‑Gln‑Lys‑Ala‑Phe‑Val‑Gln‑Trp‑Leu‑Ile‑Ala‑Gly‑Gly‑Pro‑Ser‑Ser‑Gly‑Ala‑Pro‑Pro‑Pro‑Ser‑NH₂
Solubility Soluble in dilute acetic acid, DMSO, and water (pH 3–4)
Log P (calculated) –1.3 (pH 7.4)
Isoelectric point (pI) ~5.4
Aggregation tendency Low in acidic buffers (pH 3–4); avoid neutral/alkaline pH

3. Mechanism of Action (API Level)

Tirzepatide functions as an unbalanced, biased dual agonist with high affinity for both human GIP and GLP‑1 receptors. At the molecular level:

  • GIP receptor activation: Enhances glucose‑dependent insulin secretion, improves peripheral insulin sensitivity, and modulates lipid metabolism in adipose tissue.

  • GLP‑1 receptor activation: Augments insulin secretion, suppresses glucagon release, delays gastric emptying, and reduces appetite via central nervous system pathways.

The dual activation produces synergistic metabolic benefits beyond those of pure GLP‑1 agonists. The GIP component also counteracts GLP‑1‑induced nausea and emesis in preclinical models, potentially improving tolerability.

4. Pharmaceutical Applications

Tirzepatide API is used in the manufacture of finished injectable drug products for the following therapeutic areas:

4.1 Type 2 Diabetes Mellitus (T2DM)

  • Improves glycemic control (HbA1c reduction) as monotherapy or in combination with metformin, SGLT2 inhibitors, or sulfonylureas.

  • Low risk of hypoglycemia due to glucose‑dependent insulin secretion.

4.2 Chronic Weight Management (Obesity/Overweight)

  • Indicated for adults with BMI ≥ 30 kg/m², or BMI ≥ 27 kg/m² with at least one weight‑related comorbidity (hypertension, dyslipidemia, obstructive sleep apnea, cardiovascular disease).

  • Used in conjunction with reduced‑calorie diet and increased physical activity.

4.3 Obstructive Sleep Apnea (OSA)

  • Approved for moderate‑to‑severe OSA in adults with obesity.

4.4 Investigational / Pipeline

  • Non‑alcoholic steatohepatitis (NASH / MASH)

  • Heart failure with preserved ejection fraction (HFpEF)

  • Cardiovascular risk reduction in high‑risk populations

5. Product Specifications (Typical)

Test Specification (Pharmaceutical Grade)
Appearance White to off‑white lyophilized cake or powder
Identification (HPLC/MS) Retention time and mass spectrum match reference standard
Purity (HPLC, area %) ≥99.0%
Single largest impurity ≤0.5%
Total related impurities ≤1.0%
Peptide content (anhydrous) 70.0–85.0%
Water content (KF) ≤6.0%
Acetate content (IC) 5.0–12.0%
Residual solvents (Class 3) ≤0.5% each
Bacterial endotoxins <5 EU/mg
Sterility (if sterile‑filtered) Compliant

Research grade material (≥98% purity) is available for early discovery and screening.

6. Advantages of Aozunchem’s Tirzepatide API

  • High synthetic purity – ≥99.0% by HPLC, fully characterized by MS, amino acid analysis, and peptide mapping.

  • Stable supply chain – cGMP‑like manufacturing with batch‑to‑batch consistency.

  • Complete documentation – COA, MSDS, TDS, and stability data provided.

  • Flexible packaging – 100 mg, 500 mg, 1 g, 5 g, 10 g, and bulk quantities.

  • Cold‑chain shipping – Shipped on dry ice or with refrigerated gel packs (‑20 °C or 2–8 °C as required).

  • Regulatory support – DMF (Drug Master File) available for qualified customers.

7. Packaging & Storage

Container Quantity Condition
Type I glass vial with rubber stopper and flip‑off seal 100 mg, 500 mg, 1 g Double‑bagged, under nitrogen
Larger vials or sterile bags 5 g, 10 g, 50 g Upon request

Storage: Store at −20 ± 5 °C in a freezer. Avoid repeated freeze‑thaw cycles (max 2 cycles). Protect from light and moisture. Under recommended storage, stability is at least 24 months from manufacture date.

Stability summary:

  • −20 °C: ≥24 months

  • 2–8 °C: 3–6 months (short‑term handling)

  • 25 °C: ≤30 days (for formulation processing)

8. Frequently Asked Questions (FAQs)

8.1 General Questions

Q1: What is the CAS number of tirzepatide?
Tirzepatide has CAS number 2023788-19-2. This number identifies the peptide base (without salt form). The acetate salt (most common API form) is covered under the same CAS registry.

Q2: What is the difference between tirzepatide and semaglutide?
Tirzepatide is a dual GIP/GLP‑1 receptor agonist, while semaglutide is a selective GLP‑1 receptor agonist. In clinical trials, tirzepatide demonstrated superior weight loss and HbA1c reduction compared to semaglutide. The dual mechanism is believed to provide additional metabolic benefits and potentially better gastrointestinal tolerability.

Q3: Does tirzepatide have a black box warning?
Yes. The finished drug product carries a black box warning regarding thyroid C‑cell tumors (medullary thyroid carcinoma, MTC) observed in rat studies. The API itself is not directly hazardous in this respect, but the warning applies to final medicinal products. Tirzepatide should not be used in patients with personal or family history of MTC or with Multiple Endocrine Neoplasia syndrome type 2 (MEN‑2).

8.2 Quality & Specifications

Q4: What is the purity of your tirzepatide API?
We offer two grades: Research grade (≥98% purity by HPLC) and Pharmaceutical grade (≥99% purity). All batches include a detailed Certificate of Analysis (COA) listing impurities, water content, acetate content, and peptide assay.

Q5: What impurities are typically monitored in tirzepatide API?
Common related substances include deamidated products (Asn → Asp), oxidation products (Trp oxidation), truncated sequences, and missing acyl side‑chain variants. Our specification limits each impurity to ≤0.5% and total impurities to ≤1.0% for pharmaceutical grade.

Q6: Can you supply tirzepatide for clinical trial use?
Yes. Aozunchem supplies tirzepatide API under appropriate quality systems for Phase I–III clinical trials. Documentation includes a drug master file (DMF) reference, stability data, and manufacturing records. Please contact us to discuss your specific regulatory requirements.

8.3 Handling, Storage & Stability

Q7: How should tirzepatide powder be stored and handled?
Store at −20 °C in the original container, tightly closed, protected from light. Allow the vial to warm to room temperature before opening to avoid moisture condensation. Reconstitute in slightly acidic aqueous buffer (e.g., 0.1% acetic acid or PBS at pH 3–4) for stock solutions. Avoid vigorous shaking.

Q8: What is the solubility of tirzepatide?
Tirzepatide is soluble in water at low pH (3–4) up to 10 mg/mL. It is also soluble in dilute acetic acid (0.1–1%) and DMSO. Solubility greatly decreases at neutral or alkaline pH due to aggregation. For subcutaneous injection formulations, the pH is typically adjusted to 6.0–7.0 using buffers and excipients to maintain solubility.

Q9: What are the primary degradation pathways of tirzepatide?
In solution, tirzepatide degrades mainly via deamidation at asparagine residues, aggregation at neutral pH, and oxidation of tryptophan. Lyophilized solid is stable for years at −20 °C. For liquid formulations, antioxidants and chelators are commonly added.

Q10: What is the recommended reconstitution buffer for in‑vivo studies?
For animal studies, reconstitute the lyophilized powder in sterile water for injection containing 0.1% acetic acid or 10 mM citrate buffer (pH 3.5), then dilute to final concentration with phosphate‑buffered saline (PBS) or normal saline at pH 7.4. The final pH should be checked (target ~6.5–7.0) and the solution used within a few hours if kept at room temperature, or within 24 h if stored at 2–8 °C.

8.4 Ordering & Support

Q11: Do you offer smaller quantities for R&D testing?
Yes. Sample quantities from 10 mg to 100 mg are available for early‑stage research and analytical method development. Please request a quote with your intended application.

Q12: Is tirzepatide a controlled substance?
No. Tirzepatide is not listed as a controlled substance under international drug control conventions. However, it is a prescription-only drug in finished dosage form and requires proper handling as a potent bioactive peptide.

9. Contact Us

For pricing, technical data sheets (TDS/MSDS), sample requests, or to request a DMF and regulatory documentation for tirzepatide API:

Email: [email protected]
WeChat / WhatsApp: +86 186 5121 5887