Tirzepatide (LY3298176) sodium

製品コードP1206 バッチP120603

印刷

化学情報

Chemical Structure Synonyms Storage
(From the date of receipt)		 3 years-20°C powder
化学式

C225H348N48O68• XNa
分子量 4813.45 CAS No. 2023788-19-2 (free base)
Solubility (25°C)* 体外 DMSO 100 mg/mL (20.77 mM)
Ethanol 3 mg/mL (0.62 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.
in vitro

In HEK293 cells, Tirzepatide induces internalization of the GIPR and has a propensity toward partial agonism, and this ultimately reflects in signaling bias toward the cAMP pathway versus β-arrestin recruitment.[1]
in vivo

LY3298176 shows glucose-dependent insulin secretion and improves glucose tolerance by acting on both GIP and GLP-1 receptors in mice. Chronic treatment with LY3298176 results in a significant dose-dependent decrease in body weight that is more pronounced than that observed with semaglutide.[2]
密度 95.0~105.0%

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK293 cells
濃度 1 nM, 10 nM, 100 nM, 1 μM
反応時間 60 min
実験の流れ
動物実験 動物モデル Mouse
投薬量 10 nmoL/kg, 30 nmoL/kg, 100 nmoL/kg
投与方法 s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/32730231/
  • https://pubmed.ncbi.nlm.nih.gov/30473097/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Proinflammatory cytokine-induced alpha cell impairment in human islet microtissues is partially restored by dual incretin receptor agonism [ Diabetologia, 2025, 10.1007/s00125-025-06425-3] PubMed: 40374968
Tirzepatide, a dual GIP/GLP-1 receptor agonist, alleviates metabolic dysfunction-associated steatotic liver disease by reducing the expression of CD36 and OBP2A [ Genes Dis, 2025, 12(6):101761] PubMed: 40837406
Evidence that tirzepatide protects against diabetes-related cardiac damages [ Cardiovasc Diabetol, 2024, 23(1):112] PubMed: 38555463
Tirzepatide prevents neurodegeneration through multiple molecular pathways [ J Transl Med, 2024, 22(1):114] PubMed: 38287296
Adropin/Tirzepatide Combination Mitigates Cardiac Metabolic Aberrations in a Rat Model of Polycystic Ovarian Syndrome, Implicating the Role of the AKT/GSK3β/NF-κB/NLRP3 Pathway [ Int J Mol Sci, 2024, 26(1)1] PubMed: 39795860
GLP-1/GIP dual agonist tirzepatide normalizes diabetic nephropathy via PI3K/AKT mediated suppression of oxidative stress [ Int Immunopharmacol, 2024, 146:113877] PubMed: 39700965
Tirzepatide attenuates mammary tumor progression in diet-induced obese mice [ bioRxiv, 2024, 2024.01.20.576484] PubMed: 38328151
Tirzepatide attenuates mammary tumor progression in diet-induced obese mice [ bioRxiv, 2024, 23:2024.01.20.576484.] PubMed: 38328151
Protection of pancreatic islets from oxidative cell death by a peripherally-active morphinan with increased drug safety [ Mol Metab, 2023, 75:101775] PubMed: 37451343
Tirzepatide inhibits tumor growth in mice with diet-induced obesity [ bioRxiv, 2023, 10.1101/2023.06.22.546093] PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。