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For research use only. Not for human consumption.

G2-T 30MG research vial, 3rd Rock Compounds

Front label

Metabolic | >99.80% purity

G2-T 30MG

  • Tirzepatide
  • LY3298176
  • GIP/GLP-1 RA
  • Twincretin

Tirzepatide (also known as LY3298176 ) is a first-in-class, synthetic 39-amino acid peptide engineered as a dual agonist for both the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor.

Strength

10MG$6520MG$8030MG$14060MG$275

$140

Lot

T26C856

Purity (HPLC-UV/VIS)

>99.80%

Lab

Vanguard Laboratory

View certificate of analysis →

Issued by Vanguard Laboratory, A2LA #6377.01.01. Testing was commissioned by our fulfilment partner on the material we ship; the certificate names that party, not 3rd Rock Compounds.

Quantity

G2-T 30MG

1 vial · $140

  • Third-party HPLC tested
  • Lot-matched certificate
  • Same-day fulfilment before 2pm
  • Shipping 2–4 business days

Identifiers

CAS number
2023788-19-2
Molecular formula
C₂₂₅H₃₄₈N₄₈O₆₈
Molecular weight
4813.53 Da
PubChem CID
166567236
Sequence
Tyr-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Aib-Leu-Asp-Lys(C20 fatty diacid)-Ile-Ala-Gln-Lys-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH₂

Mechanism of Action

Tirzepatide is a first-in-class unimolecular dual agonist that simultaneously targets the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor. [1] It functions as an imbalanced agonist: binding affinity for the GIP receptor equals that of native GIP, while GLP-1 receptor affinity is approximately 5- to 13-fold weaker than native GLP-1. [6] Cryo-electron microscopy confirms the N-terminus of tirzepatide (Tyr1) forms hydrogen bonds with GLP-1R residues (e.g., Gln234), while Glu3 forms ionic bonds with Arg190, with analogous interactions at the GIPR. [8]

2. Biased Agonism — cAMP Over β-Arrestin

Unlike native GLP-1 which recruits both G-proteins and β-arrestin, tirzepatide exhibits biased agonism at the GLP-1 receptor: it preferentially activates cyclic adenosine monophosphate (cAMP) generation while inducing significantly lower β-arrestin recruitment. [9] This reduces receptor internalization and desensitization, maintaining GLP-1R availability at the cell surface for prolonged signaling. At the GIP receptor, tirzepatide mimics the signaling profile of native GIP. [10]

3. Downstream Signaling — cAMP/PKA, PI3K/AKT, AMPK, NF-κB

Binding to GIP/GLP-1 receptors initiates several key intracellular cascades: [11]

  • cAMP/PKA Pathway: Upregulated intracellular cAMP activates Protein Kinase A, stimulating glucose-dependent insulin secretion from pancreatic β-cells.
  • PI3K/AKT Pathway: Enhances mitochondrial function, reduces neuroinflammation, and promotes cell survival.
  • AMPK Pathway: Activated in CNS and peripheral tissues, linked to metabolic regulation and energy homeostasis.
  • NF-κB Inhibition: Suppresses the TLR4/NF-κB/NLRP3 inflammasome pathway, reducing pro-inflammatory cytokines (TNF-α, IL-6). [12]
  • CREB/BDNF Pathway: In neuronal cells, activates pAkt/CREB/BDNF signaling to promote neuronal growth and survival. [13]

4. Tissue-Level Effects

Pancreas: Enhances both first- and second-phase insulin secretion in a glucose-dependent manner. Reduces fasting and postprandial glucagon secretion during hyperglycemia while preserving glucagonotropic function during hypoglycemia. [14]

Adipose Tissue: GIP receptor agonism improves insulin sensitivity in adipose tissue, increases adiponectin levels by 16–26%, and enhances lipid buffering via increased lipoprotein lipase (LPL) activity. [15]

CNS: Acts on the hypothalamus to regulate appetite and satiety. Animal research (Bossi et al., 2025) indicates tirzepatide temporarily increases energy expenditure shortly after dosing, unlike semaglutide which initially reduces it. [16]

Liver: Reduces liver fat content and stiffness; in the SYNERGY-NASH trial, resolved MASH without worsening fibrosis in up to 62% of participants. [17]

5. Pharmacokinetics — Once-Weekly Dosing

The C20 fatty diacid enables 99% albumin binding, yielding a half-life of ~5 days (116.7 hours), bioavailability of ~80% SC, Tmax of 8–72 hours, and Vd of ~10.3 L. [3] Metabolism occurs via proteolytic cleavage, β-oxidation of the fatty diacid moiety, and amide hydrolysis. Metabolites are excreted via urine and feces. [18]

6. Dose-Response Relationships

Clinical trials demonstrate clear dose-dependent efficacy across all indications: [19]

  • HbA1c (SURPASS-1): −1.87% (5 mg), −1.89% (10 mg), −2.07% (15 mg)
  • Weight loss (SURMOUNT-1): −15.0% (5 mg), −19.5% (10 mg), −20.9% (15 mg)
  • MASH resolution (SYNERGY-NASH): 44% (5 mg), 56% (10 mg), 62% (15 mg)

Preclinical Research Findings

Tirzepatide has been studied across the SURPASS clinical trial program (SURPASS-1 through SURPASS-6, plus SURPASS-CVOT) in over 17,000 study subjects with type 2 diabetes mellitus (T2DM). In SURPASS-2 (n=1,879), tirzepatide demonstrated superiority over semaglutide 1 mg, with HbA1c reductions of −2.01% to −2.30% vs. −1.86%, and weight loss of −7.6 to −11.2 kg vs. −5.7 kg. [7] The landmark SURPASS-CVOT (n=13,299) confirmed cardiovascular tolerability with a MACE HR of 0.92 vs. dulaglutide. [20]

⚖️ Obesity & Weight Management (SURMOUNT Program)

In the pivotal SURMOUNT-1 trial (n=2,539 adults with obesity, without T2DM), tirzepatide produced weight reductions of −15.0% (5 mg), −19.5% (10 mg), and −20.9% (15 mg) at 72 weeks vs. −3.1% with placebo. [21] The 3-year SURMOUNT-1 extension showed sustained weight reduction (−12.3% to −19.7%) and observed changes in metabolic markers in preclinical and research settings (HR 0.07). [22]

In the head-to-head SURMOUNT-5 trial (n=751), tirzepatide achieved −20.2% weight loss vs. −13.7% for semaglutide 2.4 mg, establishing superiority. [23]

See also: AOD-9604 for related weight management research.

❤️ Heart Failure (SUMMIT Trial)

The SUMMIT trial (n=731) investigated tirzepatide in study subjects with heart failure with preserved ejection fraction (HFpEF) and obesity, showing a 38% reduction in risk of CV death/worsening heart failure (HR 0.62) and 6.9-point greater improvement in KCCQ-CSS (Kansas City Cardiomyopathy Questionnaire). [24]

💤 Obstructive Sleep Apnea (SURMOUNT-OSA)

The SURMOUNT-OSA trials (n=469) demonstrated that tirzepatide reduced the apnea-hypopnea index (AHI) by up to 62.8% (−25.3 to −29.3 events/hr vs. −5.3 to −5.5 placebo) in study subjects with moderate-to-severe OSA and obesity. FDA approval for an OSA indication was granted in December 2024. [25]

🫁 Liver Disease (SYNERGY-NASH)

In the Phase 2 SYNERGY-NASH trial (n=190), tirzepatide achieved MASH resolution without worsening fibrosis in 44% (5 mg), 56% (10 mg), and 62% (15 mg) vs. 10% placebo. Fibrosis improvement (≥1 stage) occurred in ~51–55% of tirzepatide groups vs. 30% placebo. [17]

🧠 Neuroprotection (Preclinical)

Preclinical studies suggest tirzepatide may have neuroprotective effects in Alzheimer’s and Parkinson’s disease models. In APP/PS1 mice (Alzheimer’s model), tirzepatide reduced amyloid-beta plaque density, decreased astrocytic activation, and reduced neuronal ROS production. [26] In neuroblastoma cells, it prevented high-glucose-induced neurodegeneration via CREB/BDNF pathway modulation. [13]

🫀 Kidney Protection (Exploratory)

Exploratory analyses from SURPASS-4 indicate tirzepatide may delay eGFR decline and reduce albuminuria compared to insulin glargine, prompting ongoing studies targeting chronic kidney disease outcomes. [27]

Safety Profile

Findings summarised above derive from in-vitro and animal studies. No safety profile for human use is established or implied, and none is offered here.

Handle as a laboratory reagent: avoid inhalation and contact, reconstitute under aseptic conditions, and observe the storage conditions below.

For research use only. Not for human consumption.

Shipping and Storage

  • Supplied as lyophilised powder in a sealed vial.
  • Store at 2–8°C (36–46°F). Protect from light.
  • Same-day fulfilment on orders before 2pm; shipping 2–4 business days.
  • For research use only. Not for human consumption.

References

  1. [1]Frías JP, Davies MJ, Rosenstock J, et al. Tirzepatide versus Semaglutide Once Weekly in study subjects with Type 2 Diabetes. N Engl J Med, 385(6), 503–515, 2021. PubMed →
  2. [2]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, 12(1), 143–157, 2021. PubMed →
  3. [3]Chavda VP, Ajabiya J, Teli D, et al. Tirzepatide, a New Era of Dual-Targeted research application for Diabetes and Obesity: A Mini-Review. Molecules, 27(13), 4315, 2022.
  4. [4]U.S. FDA. MOUNJARO® (tirzepatide) Injection — Prescribing Information. FDA Access Data, 2022. accessdata.fda.gov →
  5. [5]U.S. FDA. ZEPBOUND® (tirzepatide) Injection — Prescribing Information. FDA Access Data, 2024. accessdata.fda.gov →
  6. [6]Liu QK. Mechanisms of action and experimental applications of GLP-1 and dual GIP/GLP-1 receptor agonists. Front Endocrinol, 15, 1431292, 2024.
  7. [7]Frías JP, Davies MJ, Rosenstock J, et al. Tirzepatide versus Semaglutide Once Weekly in study subjects with Type 2 Diabetes. N Engl J Med, 385(6), 503-515, 2021. PubMed →
  8. [8]Coskun T, Sloop KW, Loghin C, et al. LY3298176, a novel dual GIP and GLP-1 receptor agonist for the investigation of type 2 diabetes mellitus: From discovery to clinical proof of concept. Mol Metab, 18, 3–14, 2018. PubMed →
  9. [9]Sun B, Willard FS, Bhavsar S, et al. Tirzepatide’s biased agonism at the GLP-1 receptor. Signal Transduction Res, 2022. PubMed →
  10. [10]Geisler CE, Antonellis MP, Trumbauer W, et al. Tirzepatide suppresses palatable food intake by selectively reducing preference for fat in rodents. Diabetes Obes Metab, 25(1), 56–67, 2022.
  11. [11]Ghaleb J, Khouzami KK, Nassif N, et al. Unveiling Tirzepatide’s experimental Spectrum: A Dual GIP/GLP-1 Agonist Targeting Metabolic, Neurological, and Cardiovascular Health. Int J Endocrinol, 2025, 2876156, 2025.
  12. [12]Liu C, et al. Tirzepatide attenuates lipopolysaccharide-induced cardiomyopathy via inhibiting TLR4/NF-κB/NLRP3 pathway. 2023.
  13. [13]Fontanella RA, Ghosh P, Pesapane A, et al. Tirzepatide prevents neurodegeneration through multiple molecular pathways. J Transl Med, 22, 114, 2024.
  14. [14]Rosenstock J, Wysham C, Frías JP, et al. Efficacy and tolerability of tirzepatide in study subjects with type 2 diabetes (SURPASS-1). Lancet, 398(10295), 143–155, 2021.
  15. [15]Del Prato S, Kahn SE, Pavo I, et al. Tirzepatide versus insulin glargine in type 2 diabetes and increased cardiovascular risk (SURPASS-4). Lancet, 398(10313), 1811–1824, 2021. PubMed →
  16. [16]Bossi AC, et al. Animal research reveals metabolic differences between tirzepatide and semaglutide. 2025. news-medical.net →
  17. [17]Loomba R, Hartman ML, Lawitz EJ, et al. Tirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis. N Engl J Med, 391(4), 299–310, 2024. PubMed →
  18. [18]European Medicines Agency. Mounjaro (tirzepatide) — Summary of Product Characteristics. EMA, 2023. ema.europa.eu →
  19. [19]Rosenstock J, Wysham C, Frías JP, et al. Efficacy and tolerability of tirzepatide in study subjects with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial. Lancet, 398(10295), 143–155, 2021.
  20. [20]Nicholls SJ, Pavo I, Bhatt DL, et al. Cardiovascular outcomes with tirzepatide versus dulaglutide in type 2 diabetes. N Engl J Med, 393, 2409–2420, 2025.
  21. [21]Jastreboff AM, Aronne LJ, Ahmad NN, et al. Tirzepatide Once Weekly for the investigation of Obesity. N Engl J Med, 387(3), 205–216, 2022. PubMed →
  22. [22]Jastreboff AM, le Roux CW, Stefanski A, et al. Tirzepatide for Obesity research application and Diabetes Prevention. N Engl J Med, 392(10), 958–971, 2025.
  23. [23]Aronne LJ, Horn DB, le Roux CW, et al. Tirzepatide as Compared with Semaglutide for the investigation of Obesity. N Engl J Med, 393(1), 26–36, 2025.
  24. [24]Packer M, Zile MR, Kramer CM, et al. Tirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity. N Engl J Med, 392(5), 427–437, 2025.
  25. [25]Malhotra A, Grunstein RR, Fietze I, et al. Tirzepatide for the investigation of Obstructive Sleep Apnea and Obesity. N Engl J Med, 391, 1193–1205, 2024. PubMed →
  26. [26]Yang Y, et al. Tirzepatide demonstrates neuroprotective effects in APP/PS1 Alzheimer’s disease model. 2024.
  27. [27]Heerspink HJL, et al. Kidney outcomes with tirzepatide vs insulin glargine (SURPASS-4 exploratory analysis). Lancet Diabetes Endocrinol, 2022.
  28. [28]Geisler CE, Antonellis MP, Trumbauer W, et al. Tirzepatide suppresses palatable food intake by selectively reducing preference for fat in rodents. Diabetes Obes Metab, 25(1), 56–67, 2022.
  29. [29]U.S. FDA. MOUNJARO Prescribing Information — Carcinogenicity and Reproductive Toxicity Data. FDA, 2022. accessdata.fda.gov →
  30. [30]Garvey WT, Frías JP, Jastreboff AM, et al. Tirzepatide once weekly for the investigation of obesity in people with type 2 diabetes (SURMOUNT-2). Lancet, 402(10402), 613–626, 2023.
  31. [31]Wadden TA, Chao AM, Machineni S, et al. Tirzepatide after intensive lifestyle intervention in adults with overweight or obesity (SURMOUNT-3). Nat Med, 29(11), 2909–2918, 2023. PubMed →
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  33. [33]Ludvik B, Giorgino F, Jódar E, et al. Once-weekly tirzepatide versus once-daily insulin degludec (SURPASS-3). Lancet, 398, 583–598, 2021.
  34. [34]Dahl D, Onishi Y, Norwood P, et al. Effect of Subcutaneous Tirzepatide vs Placebo Added to Titrated Insulin Glargine (SURPASS-5). JAMA, 327(6), 534–545, 2022. PubMed →
  35. [35]Rosenstock J, Frías JP, Rodbard HW, et al. Tirzepatide vs Insulin Lispro Added to Basal Insulin (SURPASS-6). JAMA, 330(17), 1631–1640, 2023.
  36. [36]Inagaki N, et al. Efficacy and tolerability of tirzepatide in Japanese study subjects with type 2 diabetes (SURPASS-J-mono). Lancet Diabetes Endocrinol, 2022.
  37. [37]Gao L, Lee BW, Chawla M, et al. Tirzepatide versus insulin glargine in the Asia-Pacific region (SURPASS-AP-Combo). Nat Med, 29(6), 1500–1510, 2023.
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  39. [39]Angelopoulos N, et al. Short-term effects of low-dose tirzepatide on lipid profile, glucose homeostasis and hepatic steatosis index in adults with obesity. J Diabetes Complications, 39(12), 109181, 2025.
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