Tirzepatide
(Synonyms: 新型双重GIP\GLP-1,LY3298176) 目录号 : GC34840
Tirzepatide是一种双重胰高血糖素样肽-1 (GLP-1)和葡萄糖依赖性胰岛素性多肽(GIP)受体激动剂,是2型糖尿病(T2DM)的前瞻性治疗药物。
Cas No.:2023788-19-2
Sample solution is provided at 25 µL, 10mM.
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Tirzepatide, a dual glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptor agonist, is a prospective therapy for type 2 diabetes mellitus (T2DM) [1-3].
Tizepatide(0.2 µM;7days) can ameliorate high glucose-induced neurodegeneration and overcome neuronal insulin resistance[4].
Tirzepatide (10 nmol/kg;14days; s.c) remarkably reduces LPS-mediated inflammatory responses by inhibiting the cardiac protein levels of TNF-α, IL-6, and IL-1B in mice[5]. Tirzepatide(3-10 nmol/kg;14days; s.c) enhances insulin sensitivity in obese mice[6]. Tirzepatide had anti-allergic inflammatory effects for the aeroallergen-induced model in obese asthma[7]. Tirzepatide improves beta-cell function and insulin sensitivity in type 2 diabetes[8].
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]. Coskun T, Sloop KW, 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. 2018 Dec;18:3-14. doi: 10.1016/j.molmet.2018.09.009. Epub 2018 Oct 3. PMID: 30473097; PMCID: PMC6308032.
[3]. Forzano I, Varzideh F, et,al. Tirzepatide: A Systematic Update. Int J Mol Sci. 2022 Nov 23;23(23):14631. doi: 10.3390/ijms232314631. PMID: 36498958; PMCID: PMC9741068.
[4]. Fontanella RA, Ghosh P, et, al. Tirzepatide prevents neurodegeneration through multiple molecular pathways. J Transl Med. 2024 Jan 29;22(1):114. doi: 10.1186/s12967-024-04927-z. PMID: 38287296; PMCID: PMC10823712.
[5]. Liu Q, Zhu J, et,al. Tirzepatide attenuates lipopolysaccharide-induced left ventricular remodeling and dysfunction by inhibiting the TLR4/NF-kB/NLRP3 pathway. Int Immunopharmacol. 2023 Jul;120:110311. doi: 10.1016/j.intimp.2023.110311. Epub 2023 May 15. PMID: 37196559.
[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]. Toki S, Zhang J, et,al. Dual GIPR and GLP-1R agonist tirzepatide inhibits aeroallergen-induced allergic airway inflammation in mouse model of obese asthma. Clin Exp Allergy. 2023 Feb;53(2):216-221. doi: 10.1111/cea.14252. Epub 2022 Nov 15. PMID: 36377605; PMCID: PMC10163938.
[8]. Thomas MK, Nikooienejad A, et,al. Dual GIP and GLP-1 Receptor Agonist Tirzepatide Improves Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes. J Clin Endocrinol Metab. 2021 Jan 23;106(2):388-396. doi: 10.1210/clinem/dgaa863. PMID: 33236115; PMCID: PMC7823251.
Tirzepatide是一种双重胰高血糖素样肽-1 (GLP-1)和葡萄糖依赖性胰岛素性多肽(GIP)受体激动剂,是2型糖尿病(T2DM)的前瞻性治疗药物[1-3]。
Tirzepatide (0.2 µM;7d)可改善高糖诱导的神经变性,克服神经元胰岛素抵抗[4]。
Tirzepatide(10 nmol/kg;14days; s.c)通过抑制小鼠心肌蛋白TNF-α、IL-6和IL-1B水平显著降低LPS介导的炎症反应[5]。Tirzepatide(3-10 nmol/kg;14days; s.c)慢性治疗可增强肥胖小鼠的胰岛素耐量[6]。Tirzepatide对空气变应原诱导的肥胖哮喘模型具有抗变应性炎症作用[7]。Tirzepatide改善2型糖尿病的β细胞功能和胰岛素敏感性[8]。
| Cell experiment [1]: | |
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Cell lines |
SHSY5Y human neuroblastoma cell line |
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Preparation Method |
The cells were exposed to normal (NG) and high glucose (HG) for 7 days. Both NG and HG cells, after reaching 70-80% of confluence, were treated with Tirzepatide at concentration of 0.2 µM. |
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Reaction Conditions |
0.2 µM Tirzepatide;7days |
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Applications |
Tirzepatide increases the growth markers expression in neuronal cells exposed to HG. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
Obese insulin-resistant mice were dosed once daily for 14 days with vehicle or tirzepatide. |
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Dosage form |
3-10 nmol/kg;14days; s.c |
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Applications |
Tirzepatide enhances insulin sensitivity. |
|
References: [1]. Fontanella RA, Ghosh P, et, al. Tirzepatide prevents neurodegeneration through multiple molecular pathways. J Transl Med. 2024 Jan 29;22(1):114. doi: 10.1186/s12967-024-04927-z. PMID: 38287296; PMCID: PMC10823712. | |
| Cas No. | 2023788-19-2 | SDF | |
| 别名 | 新型双重GIP\GLP-1,LY3298176 | ||
| 分子式 | C225H348N48O68 | 分子量 | 4813.45 |
| 溶解度 | DMSO : 50 mg/mL (10.39 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.2078 mL | 1.0388 mL | 2.0775 mL |
| 5 mM | 0.0416 mL | 0.2078 mL | 0.4155 mL |
| 10 mM | 0.0208 mL | 0.1039 mL | 0.2078 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet