Tirzepatide hydrochloride (Synonyms: LY3298176 hydrochloride) |
رقم الكتالوجGC38132 |
هيدروكلوريد تيرزيباتيد (LY3298176 هيدروكلوريد) هو متعدد الببتيد الأنسولين المعتمد على الجلوكوز (GIP) ونهض مستقبلات الببتيد 1 (GLP-1) الذي يشبه الجلوكاجون والذي يتم تطويره لعلاج مرض السكري من النوع 2.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
Tirzepatide is a dual GIP and GLP-1 receptor agonist that has demonstrated improved glycemic control and superior weight loss. Tirzepatide induces the internalization of GIP and GLP-1 receptors in different ways, with EC50 values of 18.2 nM and 18.1 nM, respectively [1-4].
After tirzepatide treatment(10 nmol/kg; s.c.;3 or 14-days), the weight and food intake of mice were significantly reduced[5]. Chronic treatment with tirzepatide (10 nmol/kg; s.c.; 14-days) enhanced insulin tolerance in obese mice[6]. In mice and rats, treatment with tirzepatide(0.3, 1, 3, 10 and 30 nmol/kg; s.c.; 14-days) simultaneously reduced the intake of a palatable high-fat/high-sugar diet and increased the consumption of a low-fat chow diet[7].
References:
[1]. Willard FS, Douros JD, et,al. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight. 2020 Sep 3;5(17):e140532. doi: 10.1172/jci.insight.140532. PMID: 32730231; PMCID: PMC7526454.
[2].Nauck MA, D'Alessio DA. Tirzepatide, a dual GIP/GLP-1 receptor co-agonist for the treatment of type 2 diabetes with unmatched effectiveness regrading glycaemic control and body weight reduction. Cardiovasc Diabetol. 2022 Sep 1;21(1):169. doi: 10.1186/s12933-022-01604-7. PMID: 36050763; PMCID: PMC9438179.
[3]. Frías JP. Tirzepatide: a glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) dual agonist in development for the treatment of type 2 diabetes. Expert Rev Endocrinol Metab. 2020 Nov;15(6):379-394. doi: 10.1080/17446651.2020.1830759. Epub 2020 Oct 8. PMID: 33030356.
[4]. Frías JP, Davies MJ, et,al. Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes. N Engl J Med. 2021 Aug 5;385(6):503-515. doi: 10.1056/NEJMoa2107519. Epub 2021 Jun 25. PMID: 34170647.
[5]. Samms RJ, Zhang G, et,al. Tirzepatide induces a thermogenic-like amino acid signature in brown adipose tissue. Mol Metab. 2022 Oct;64:101550. doi: 10.1016/j.molmet.2022.101550. Epub 2022 Jul 31. PMID: 35921984; PMCID: PMC9396640.
[6]. Samms RJ, Christe ME, et,al. GIPR agonism mediates weight-independent insulin sensitization by tirzepatide in obese mice. J Clin Invest. 2021 Jun 15;131(12):e146353. doi: 10.1172/JCI146353. PMID: 34003802; PMCID: PMC8203452.
[7]. Geisler CE, Antonellis MP, et,al. Tirzepatide suppresses palatable food intake by selectively reducing preference for fat in rodents. Diabetes Obes Metab. 2023 Jan;25(1):56-67. doi: 10.1111/dom.14843. Epub 2022 Sep 12. PMID: 36054312; PMCID: PMC10362946.
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