Tirzepatide 10mg

Tirzepatide is a modified-chain synthetic peptide that represents the first dual GIP (glucose-dependent insulinotropic polypeptide) and GLP-1 (glucagon-like peptide-1) receptor agonist. Its approximate molecular weight is 4,813 Da, with a half-life of 5 days documented in the literature.

Molecular design:

• Human GLP-1 derived basic scaffold
• 39 amino acids with strategic modifications for receptor duality
• Acyl chain C20 conjugated at a specific position to extend half-life
• Serum albumin binding greater than 98%, which protects against enzymatic degradation

The compound exhibits a slightly unbalanced affinity for GIP, a characteristic that appears to be responsible for the superior response observed with pure GLP-1 agonists like Semaglutide. Phase 3 trials SURPASS-1 through SURPASS-5 established its benchmark pharmacological profile.

Tirzepatide simultaneously activates two incretin pathways that normally operate in a coordinated manner in post-prandial physiology:

Via GLP-1:

• Increase glucose-dependent insulin secretion from pancreatic beta cells
• Suppress glucagon secretion from alpha cells
• Slows gastric emptying, prolonging post-meal satiety
• It acts on hypothalamic nuclei (arcuate, paraventricular) to modulate appetite

Via GIP:

• Enhance GLP-1 induced insulin secretion
• It modulates lipid metabolism in adipose tissue
• Improves the allocation of nutrients between oxidation and storage
• Reduce low-grade inflammation in visceral adipose tissue

The combination produces a documented synergistic effect: simultaneous activation of both receptors generates a greater metabolic response than the sum of each component separately, especially in terms of fat mass loss with relative preservation of lean mass.

The compound is widely investigated in the following contexts:

• Obesity Research: SURMOUNT-1 through SURMOUNT-4 reported an average reduction in body weight of 15 to 22% at 72 weeks with doses of 10 to 15 mg/week
• Type 2 diabetes SURPASS-1 to SURPASS-5 established HbA1c reductions greater than those observed with Semaglutide
• Fatty liver disease Phase 2 trials show significant reduction in liver lipid content
• Hypertension associated with obesity: average reductions of 6 to 8 mmHg in systolic pressure
• Sleep apnea: SURMOUNT-OSA showed improvement in the apnea-hypopnea index
• Cardiovascular Research: SURPASS-CVOT ongoing evaluating major outcomes

Reconstitution

Add 2 ml of bacteriostatic water to the 10 mg vial, allowing the liquid to run slowly down the inner wall of the vial. Homogenize with gentle swirling motion, do not shake. Store refrigerated between 2 and 8°C.

Resulting concentration: 5,000 mcg/mL or 5 mg/mL.

In volumetric reference with a U-100 laboratory syringe, each unit on the scale is equivalent to 50 mcg.

Reference volumetric chart (U-100 scale):

• 2.5 mg → 50 units of U-100 scale
• 5.0 mg → 100 units U-100 scale
• 7.5 mg → 150 units of U-100 scale
• 10.0 mg → 200 units U-100 scale
• 12.5 mg → 250 units on the U-100 scale
• 15.0 mg → 300 units on the U-100 scale

A 10-mg vial provides 10 mg of the compound for research preparations at the specified concentration.

Adverse events commonly reported in clinical trial literature:

• Gastrointestinal: nausea (20-30%), diarrhea, constipation, dyspepsia
• Decreased appetite

Less common but relevant events reported in the literature: acute pancreatitis (rare), hypersensitivity reactions, cholelithiasis associated with rapid weight loss.

Documented contraindications in clinical literature:

• Personal or family history of medullary thyroid carcinoma
• Multiple Endocrine Neoplasia Type 2 (MEN 2) Syndrome
• Active pancreatitis or history of severe pancreatitis
• Pregnancy and breastfeeding

Relevant documented drug interactions: delayed gastric emptying may alter the absorption of oral contraceptives and other gastric rate-sensitive drugs.

Tirzepatide is frequently studied alongside other compounds in research protocols depending on the study objective:

• Body recomposition Tirzepatide + CJC No DAC + Ipamorelin, investigated for its association with lean mass preservation during fat loss
• Fatty liver disease Tirzepatide + MOTS-C, studied for its association with mitochondrial lipid oxidation
• Metabolic Syndrome Tirzepatide + Semaglutide in crossover studies (not simultaneous)
• Leather support Tirzepatide + GHK-Cu, investigated in contexts of skin laxity associated with weight loss
• Pre-operative optimization Low-dose tirzepatide in pre-bariatric optimization research

1. Coskun T, Sloop KW, Loghin C, et al. LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus. Mol Metab. 2018;18:3-14.
2. Jastreboff AM, Aronne LJ, Ahmad NN, et al. Tirzepatide once weekly for the treatment of obesity. N Engl J Med. 2022;387(3):205-216.
3. Frías JP, Davies MJ, Rosenstock J, et al. Tirzepatide versus semaglutide once weekly in patients with type 2 diabetes. N Engl J Med. 2021;385(6):503-515.
4. Rosenstock J, Wysham C, Frías JP, et al. Efficacy and safety of tirzepatide in patients with type 2 diabetes (SURPASS-1). Lancet. 2021;398(10295):143-155.
5. Malhotra A, Grunstein RR, Fietze I, et al. Tirzepatide for the treatment of obstructive sleep apnea and obesity (SURMOUNT-OSA). N Engl J Med. 2024;391(13):1193-1205.

Product intended for scientific research purposes only. Not for human use or direct consumption. The buyer assumes full responsibility for handling the compound.