Tirzepatide hydrochloride
(Synonyms: LY3298176 hydrochloride) 目录号 : GC38132
Tirzepatide是一种双GIP和GLP-1受体激动剂，能够以不同方式诱导GIP和GLP-1受体内化，EC50值分别为18.2 nM和18.1 nM。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Animal experiment [1]: |
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Animal models |
Obese male C57/BL6J mice |
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Preparation method |
Mice received subcutaneous injections with either vehicle ( 40 mM Tris-HCl pH 8) or tirzepatide (10 nmol/kg) once a day for 3 or 14-days. |
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Dosage form |
10 nmol/kg; s.c.;3 or 14-days |
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Applications |
After tirzepatide treatment, the weight and food intake of mice were significantly reduced. |
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References: [1]. 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. |
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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.
Tirzepatide是一种双GIP和GLP-1受体激动剂，可以改善血糖控制和减轻体重。Tirzepatide以不同方式诱导GIP和GLP-1受体内化，EC50值分别为18.2 nM和18.1 nM[1-4]。
Tirzepatide治疗(10 nmol/kg; s.c.;3 or 14-days)后，小鼠体重和摄食量均显著降低[5]。Tirzepatide (10 nmol/kg; s.c.; 14-days) 慢性治疗后，可提高肥胖小鼠的胰岛素耐受性[6]。在小鼠和大鼠中，Tirzepatide治疗(0.3, 1, 3, 10 and 30 nmol/kg; s.c.; 14-days)同时减少了高脂肪/高糖饮食的摄入量，增加了低脂肪食物的摄入量[7]。
| Cas No. | SDF | ||
| 别名 | LY3298176 hydrochloride | ||
| 分子式 | C225H349N48O68Cl | 分子量 | 4849.91 |
| 溶解度 | DMSO: 100 mg/mL (20.62 mM); Water: < 0.1 mg/mL (insoluble) | 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 | 0.2062 mL | 1.0309 mL | 2.0619 mL |
| 5 mM | 0.0412 mL | 0.2062 mL | 0.4124 mL |
| 10 mM | 0.0206 mL | 0.1031 mL | 0.2062 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。