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Tirzepatide 10mg
$150.00
Products will arrive in a lyophilized (powder) form for maximum stability
Tirzepatide is a dual GLP-1/GIP receptor agonist and the first FDA-approved incretin of its class. Clinical research (SURMOUNT trials) documented greater weight and glycemic effects than single-agonist GLP-1 analogs in head-to-head comparisons. The 10mg vial format suits shorter research protocols at ≥99% HPLC purity, for research use only.
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Compound Identity
COMPOUND NAME
Tirzepatide
SYNONYMS
LY3298176
CAS NUMBER
2023788-19-2
MOLECULAR FORMULA
C225H348N48O68
MOLECULAR WEIGHT
~4813 Da
STRUCTURE
Synthetic 39-amino acid peptide
PEPTIDE SEQUENCE
His-Aib-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Aib-Leu-Asp-Lys-Glu-Glu-Glu-Glu-Ala-Gln-Aib-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH?
CHEMICAL STRUCTURE
Molecular Formula: C225H348N48O68
Molar Mass
4705 g/mol
Source: PubChem
Mechanism of Action
Tirzepatide functions as an imbalanced dual agonist of the GIP and GLP-1 receptors. It preferentially engages GIPR over GLP-1R, enhancing insulin secretion and reducing appetite. The biased agonism toward cAMP generation at the GLP-1 receptor avoids receptor internalization, contributing to increased insulinotropic effects with fewer gastrointestinal side effects at equivalent efficacy1,3.
1
GIP Receptor (GIPR) Agonism
2
Stimulates robust insulin secretion: GIPR activation enhances glucose-dependent insulin release from pancreatic beta cells, especially effective in the postprandial state2.
3
Improves lipid metabolism: Promotes lipid clearance and may support improved insulin sensitivity and adipose tissue function1,4.
4
Enhances satiety and energy balance: GIP action in the CNS contributes to reduced food intake and weight loss1,2,3.
5
Receptor binding affinity (EC?
?, Human) = ~0.135 nM
6
GLP-1 Receptor (GLP-1R) Agonism
7
Stimulates glucose-dependent insulin secretion: Enhances insulin release and lowers glucagon during hyperglycemia1.
8
Suppresses appetite (central action): Acts on hypothalamic centers to reduce hunger and increase satiety, leading to weight reduction2.
9
Slows gastric emptying: Delays nutrient absorption and moderates postprandial glucose excursions1,3.
10
Receptor binding affinity (EC?
?, Human) = ~5.4 nM
Biological Activity
Tirzepatide promotes glucose-dependent insulin secretion, reduces glucagon during hyperglycemia, increases satiety, reduces food intake, and lowers body weight. Clinical studies demonstrate substantial HbA1c reductions (up to ?2.4%) and body weight losses exceeding 20% with high-dose regimens in people with obesity and type 2 diabetes1,2.
Storage
- −20°C or below. Protect from moisture and light.
Drug Categories
Peptide therapeutics; Incretin mimetics; Dual receptor agonists.
Additional Notes
- Approved by FDA for type 2 diabetes; under investigation for obesity and NASH.
- Engineered for DPP-IV resistance and extended half-life via C20 fatty diacid modification.
Summary Table
Property
Description
CAS Number
2023788-19-2
Molecular Formula
C225H348N48O68
Molecular Weight (MW)
~4813 Da
Molar Mass
4705 g/mol
Mechanism of Action
Dual agonist at GIP and GLP-1 receptors; biased signaling, GIPR-dominant
Biological Activity
Improves glycemia, reduces weight, enhances insulin sensitivity
Supplied Form
Lyophilized powder
Purity
≥99% (HPLC)
Storage
−20°C, dry, light-protected
Drug Categories
Peptides; Incretin mimetic
Additional Notes
Long half-life, DPP-IV resistant, subcutaneous weekly dosin
Disclaimer
For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.
Detailed Product Description
Tirzepatide is a dual incretin receptor agonist engineered to activate both GIP and GLP-1 receptors, key regulators of glycemic control and energy balance. Comprising 39 amino acids with a C20 fatty diacid side chain for half-life extension, tirzepatide is designed for once-weekly subcutaneous injection. Its receptor profile is imbalanced, favoring GIPR activation, and shows biased signaling at GLP-1R to enhance insulin secretion while minimizing receptor desensitization2,5. Tirzepatide has demonstrated potent effects on lowering blood glucose and reducing body weight in patients with type 2 diabetes and obesity. Clinical trials have shown HbA1c reductions of up to 2.4% and body weight losses of up to 22.5%, with improvements in insulin sensitivity, lipid metabolism, and cardiometabolic markers2,3. These effects are dose-dependent and align with its unique receptor pharmacology and optimized pharmacokinetics. Tirzepatide is currently FDA-approved for type 2 diabetes and under evaluation for obesity and metabolic liver diseases.
Research Highlights
Superior Glycemic Control:
Tirzepatide lowers HbA1c by up to 2.4% in people with type 2 diabetes, surpassing standard therapies3,5.
Profound Weight Loss:
Up to 22.5% body weight reduction in obese individuals over 72 weeks2.
Improved Cardiometabolic Profile:
Reductions in triglycerides, blood pressure, and insulin resistance (HOMA-IR) have been observed2.
Favorable Tolerability:
Most adverse events are mild GI symptoms during titration2,3,5.
Tirzepatide exerts its dual incretin therapeutic effects through simultaneous activation of two gut hormone receptors, each contributing distinct and complementary mechanisms:
Synergy of Dual Agonism
Tirzepatide’s unique imbalanced and biased receptor activation leads to synergistic enhancement of glycemic control and body weight loss beyond what is observed with GLP-1 receptor agonists alone. The combination of GIPR dominance and GLP-1R bias toward cAMP signals results in enhanced insulin secretion, improved metabolic parameters, and a more tolerable GI side effect profile2,3,4.
Pharmacokinetic Profile
Route of Administration
Subcutaneous
Dosing Frequency
Once weekly
Half-Life
5 days
Formulation & Handling
- Store at −20°C
- Protect from light and moisture
- Reconstitute with sterile water; avoid multiple freeze-thaw cycles
Clinical Trial Activity
Trial ID
Title
Phase
Study Type
Sponsor
NCT0570650
Tirzepatide (LY3298176) in Adults With Type 2 Diabetes Switching From a GLP-1 RA (SURPASS-SWITCH-2)
4
Interventional
Eli Lilly and company
NCT0440723
A Study to Measure Stomach Emptying in Overweight Non-diabetic and Diabetic Participants Using Tirzepatide
1
Interventional
Eli Lilly and company
NCT0582283
Tirzepatide (LY3298176) in Participants With Obesity or Overweight With Weight Related Comorbidities (SURMOUNT-5)
3
Interventional
Eli Lilly and company
NCT0418462
Tirzepatide (LY3298176) in Participants With Obesity or Overweight (SURMOUNT-1)
3
Interventional
Eli Lilly and company
References
1
Willard, F.S. et al. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight 5, e140532 (2020). https://doi.org/10.1172/jci.insight.140532
2
Rosenstock, J. et al. Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial. Lancet 398, 143–155 (2021). https://doi.org/10.1016/S0140-6736(21)01324-6
3
Dahl, D. et al. Effect of Subcutaneous Tirzepatide vs Placebo Added to Titrated Insulin Glargine on Glycemic Control in Patients With Type 2 Diabetes: The SURPASS-5 Randomized Clinical Trial. JAMA 327, 534–545 (2022). https://doi.org/10.1001/jama.2022.0078
4
Jastreboff, A.M. et al. Tirzepatide Once Weekly for the Treatment of Obesity. N. Engl. J. Med. 387, 205–216 (2022). https://doi.org/10.1056/NEJMoa2206038
5
Coskun, T. et al. LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept. Mol. Metab. 18, 3–14 (2018). https://doi.org/10.1016/j.molmet.2018.09.009
Quality & Purity
This product is synthesized via solid-phase peptide synthesis (SPPS) and tested to ≥99% purity by HPLC with identity confirmed by mass spectrometry. A Certificate of Analysis (COA) is available for every batch. Learn about our full quality and testing process →
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