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Tirzepatide (5mg)

$147.00

Tirzepatide peptides are Synthesized and Lyophilized in the USA.

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Quantity5 - 910 +
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Price$139.65$132.30
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Description

What is the Tirzepatide peptide?

Tirzepatide is an analog peptide to the glucose-dependent insulinotropic polypeptide (GIP). Gastric inhibitory peptide (GIP) is a hormone produced by the duodenum and small intestine. It acts as an incretin and stimulates the production of insulin. Unlike GIP, which is made of 42 amino acids, Tirzepatide has a modified amino acid chain consisting of 39 amino acids which are additionally lipidated to improve the peptide’s uptake into cells and its stability during metabolism.[1] Tirzepatide is being investigated for its effect on type 2 diabetes, obesity, bone metabolism, the pancreas, and the central nervous system.

Specifications

Molecular Formula: C225H348N48O68

Molecular Weight: 4813.45 g/mol

Sequence: YXEGTFTSDY-SIXLDKIAQK-AFVQWLIAGG-PSSGAPPPS

Reconstitution: Required

Tirzepatide Research

Mechanism of action
Tirzepatide is a GIP-analog that activates both the GLP-1 and GIP receptors. Generally, the peptide is a more potent activator for GIP than GLP-1 receptors. Both of those receptors can be found in the pancreas but also in other organs. Usually, the small intestine produces GLP-1 and GIP when certain nutrients are in its lumen. For example, GIP is triggered by the hyperosmolarity of glucose that enters the duodenum after a meal.[2] The GIP and GLP-1 peptides are then released in the blood and travel to the corresponding receptors. Activating either of those receptors in the pancreas stimulates the beta-cells to produce insulin in a glucose-dependent manner. However, the effect is glucose-dependent, so Tirzepatide cannot trigger insulin secretion if glucose levels are low or average, and this reduces the risk of hypoglycemia. GIP receptors can also be found in the gut, adipose tissue, heart, pituitary, and inner layers of the adrenal cortex.[3] GLP-1 receptors have also been discovered in the gut, exocrine pancreas, brain, heart, lung, and kidney.[4] Thus, Tirzepatide may also have benefits other than stimulating insulin secretion, and scientists are currently exploring its potential for a wide range of conditions.

Tirzepatide and glycemic control
The main benefit of Tirzepatide is the reduction of blood sugar levels and improved glucose control in test subjects with type 2 diabetes. Studies show that due to this dual agonist behavior, Tirzepatide has the highest efficacy for improving glycemic control compared to other anti-diabetic medications such as GLP-1 agonists, SGLT-2 inhibitors, or DPP-4 inhibitors.[5] Moreover, Tirzepatide may also help improve insulin sensitivity and beta-cell function in subjects with type 2 diabetes. Studies note that the peptide reduced insulin resistance as measured by the HOMA2-IR index and the effect was more remarkable when compared to GLP-1 agonists. Thomas et al. explained that the improvement was primarily independent of body weight reduction and noted that “weight loss explained only 13% and 21% of improvement in HOMA2-IR with Tirzepatide.” [6]

Tirzepatide and weight loss
A meta-analysis of 9 studies that covered more than 7,000 test subjects with diabetes reports that Tirzepatide also leads to more weight loss than GLP-1 agonists such as Semaglutide.[7] The duration of the studies ranged from 8 to 52 weeks, and the subjects achieved about 5kg weight loss on average. Moreover, Tirzepatide led to better glycemic control than Semaglutide and insulin. Permana et al. concluded, “Tirzepatide has shown superiority in glycemic control and body weight reduction with a good safety profile in patients with T2D.” Tirzepatide has been shown to cause weight loss regardless of whether the test subject has diabetes. In one trial with 2,539 obese subjects and at least one weight-related complication, excluding diabetes, Tirzepatide led to a dramatic reduction in body weight.[8] In 72 weeks of therapy, subjects had at least a 20% reduction in body weight or more, compared to only 3% weight loss in the placebo group for the same period.

Tirzepatide and hepatoprotection
Tirzepatide has been shown to improve markers of liver function in test subjects with non-alcoholic fatty liver disease (NAFLD).[9] Apart from reducing liver enzymes such as ALT and AST, the peptide also lowered markers of liver cell death, such as K-18, and markers of liver fibrosis, such as Pro-C3.[10] Another trial reports that Tirzepatide also leads to a significant reduction in liver fat content, which is another direct marker for NAFLD.[11] In 52 weeks, the peptide led to an average 8% reduction in liver fat.

Other benefits under investigation
Tirzepatide is currently under investigation for its potential benefits for the cardiovascular system, the kidneys, and the heart.[12] In subjects with type 2 diabetes, Tirzepatide could slow the decline of kidney function and the progression of chronic kidney disease.[13] Furthermore, research reveals that Tirzepatide therapy can improve lipid profiles in subjects with diabetes. After 26 weeks, one study by Wilson et al. revealed that the peptide decreased apoB, apoC-III, LDL levels, and triglycerides. Wilson et al. report that “At 26 weeks, change in apoC-III, but not body weight, was the best predictor of changes in triglycerides with Tirzepatide, explaining up to 22.9% of their variability.”[14] The researchers also note that the improvement in the lipid profile of the subjects was partially independent of the weight loss effects of Tirzepatide.

References

  1. Ahangarpour, M., Kavianinia, I., Harris, P. W., & Brimble, M. A. (2021). Photo-induced radical thiol–ene chemistry: a versatile toolbox for peptide-based drug design. Chemical Society Reviews, 50(2), 898-944.
  2. Thorens B. (1995). Glucagon-like peptide-1 and control of insulin secretion. Diabete & metabolisme, 21(5), 311–318.
  3. Usdin, T. B., Mezey, E., Button, D. C., Brownstein, M. J., & Bonner, T. I. (1993). Gastric inhibitory polypeptide receptor, a member of the secretin-vasoactive intestinal peptide receptor family, is widely distributed in peripheral organs and the brain. Endocrinology, 133(6), 2861–2870. https://doi.org/10.1210/endo.133.6.8243312
  4. Abu-Hamdah R, Rabiee A, Meneilly GS, Shannon RP, Andersen DK, Elahi D. Clinical review: The extrapancreatic effects of glucagon-like peptide-1 and related peptides. J Clin Endocrinol Metab. 2009 Jun;94(6):1843-52. doi: 10.1210/jc.2008-1296. Epub 2009 Mar 31. PMID: 19336511; PMCID: PMC2690432.
  5. Zaazouee, M. S., Hamdallah, A., Helmy, S. K., Hasabo, E. A., Sayed, A. K., Gbreel, M. I., Elmegeed, A. A., Aladwan, H., Elshanbary, A. A., Abdel-Aziz, W., Elshahawy, I. M., Rabie, S., Elkady, S., Ali, A. S., Ragab, K. M., & Nourelden, A. Z. (2022). Semaglutide for the treatment of type 2 Diabetes Mellitus: A systematic review and network meta-analysis of safety and efficacy outcomes. Diabetes & metabolic syndrome, 16(6), 102511. https://doi.org/10.1016/j.dsx.2022.102511
  6. Thomas, M. K., Nikooienejad, A., Bray, R., Cui, X., Wilson, J., Duffin, K., Milicevic, Z., Haupt, A., & Robins, D. A. (2021). Dual GIP and GLP-1 Receptor Agonist Tirzepatide Improves Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes. The Journal of clinical endocrinology and metabolism, 106(2), 388–396. https://doi.org/10.1210/clinem/dgaa863
  7. Permana, H., Yanto, T. A., & Hariyanto, T. I. (2022). Efficacy and safety of tirzepatide as novel treatment for type 2 diabetes: A systematic review and meta-analysis of randomized clinical trials. Diabetes & metabolic syndrome, 16(11), 102640. https://doi.org/10.1016/j.dsx.2022.102640
  8. Jastreboff, A. M., Aronne, L. J., Ahmad, N. N., Wharton, S., Connery, L., Alves, B., Kiyosue, A., Zhang, S., Liu, B., Bunck, M. C., Stefanski, A., & SURMOUNT-1 Investigators (2022). Tirzepatide Once Weekly for the Treatment of Obesity. The New England journal of medicine, 387(3), 205–216. https://doi.org/10.1056/NEJMoa2206038
  9. Targher G. (2022). Tirzepatide adds hepatoprotection to its armoury. The lancet. Diabetes & endocrinology, 10(6), 374–375. https://doi.org/10.1016/S2213-8587(22)00074-2
  10. Hartman, M. L., Sanyal, A. J., Loomba, R., Wilson, J. M., Nikooienejad, A., Bray, R., Karanikas, C. A., Duffin, K. L., Robins, D. A., & Haupt, A. (2020). Effects of Novel Dual GIP and GLP-1 Receptor Agonist Tirzepatide on Biomarkers of Nonalcoholic Steatohepatitis in Patients With Type 2 Diabetes. Diabetes care, 43(6), 1352–1355. https://doi.org/10.2337/dc19-1892
  11. Gastaldelli, A., Cusi, K., Fernández Landó, L., Bray, R., Brouwers, B., & Rodríguez, Á. (2022). Effect of tirzepatide versus insulin degludec on liver fat content and abdominal adipose tissue in people with type 2 diabetes (SURPASS-3 MRI): a substudy of the randomised, open-label, parallel-group, phase 3 SURPASS-3 trial. The lancet. Diabetes & endocrinology, 10(6), 393–406. https://doi.org/10.1016/S2213-8587(22)00070-5
  12. Solini A. (2022). Tirzepatide and kidney function: an intriguing and promising observation. The lancet. Diabetes & endocrinology, 10(11), 762–763. https://doi.org/10.1016/S2213-8587(22)00258-3
  13. Heerspink, H. J. L., Sattar, N., Pavo, I., Haupt, A., Duffin, K. L., Yang, Z., Wiese, R. J., Tuttle, K. R., & Cherney, D. Z. I. (2022). Effects of tirzepatide versus insulin glargine on kidney outcomes in type 2 diabetes in the SURPASS-4 trial: post-hoc analysis of an open-label, randomised, phase 3 trial. The lancet. Diabetes & endocrinology, 10(11), 774–785. https://doi.org/10.1016/S2213-8587(22)00243-1
  14. Wilson, J. M., Nikooienejad, A., Robins, D. A., Roell, W. C., Riesmeyer, J. S., Haupt, A., Duffin, K. L., Taskinen, M. R., & Ruotolo, G. (2020). The dual glucose-dependent insulinotropic peptide and glucagon-like peptide-1 receptor agonist, tirzepatide, improves lipoprotein biomarkers associated with insulin resistance and cardiovascular risk in patients with type 2 diabetes. Diabetes, obesity & metabolism, 22(12), 2451–2459. https://doi.org/10.1111/dom.14174
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