2. GPCR/G Protein
  3. GLP Receptor GCGR
  4. TPM003

TPM003 (TG062) 是一种 GLP-1R、GIPR 和 GCGR 的三重激动剂，其 EC50 分别为 33.9、12.5 和 92.9 pM。TPM003 可抑制食欲、调控血糖、增强胰岛素敏感性、降低胃肠道不耐受性、促进肝脏脂质动员并提升能量消耗。TPM003 可诱导体重减轻、改善代谢参数、逆转肝脂肪变性并优化肝功能标志物。TPM003 可用于肥胖和非酒精性脂肪性肝炎的研究。

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TPM003

TPM003 Chemical Structure

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TPM003 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TPM003 (TG062) is a triple agonist of GLP-1R, GIPR and GCGR, with EC50 values of 33.9, 12.5 and 92.9 pM, respectively. TPM003 suppresses appetite, regulates blood glucose, enhances insulin sensitivity, reduces gastrointestinal intolerance, promotes hepatic lipid mobilization and increases energy expenditure. TPM003 induces weight loss, improves metabolic parameters, reverses hepatic steatosis and optimizes liver function markers. TPM003 is applicable for research on obesity and non-alcoholic steatohepatitis[1].

药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUC0-inf AUC0-t Cmax Tmax F
Rat[1] 1.0 mg/kg i.v. 21.5 h 289.2 μg·h/mL 265.3 μg·h/mL / / /
Rat[1] 3.0 mg/kg s.c. 26.4 h 570.3 μg·h/mL 410.5 μg·h/mL 8.2 μg/mL 24 h 50.9 %
Cynomolgus Monkey[1] 0.2 mg/kg i.v. 83.3 h 302.1 μg·h/mL 277.6 μg·h/mL / / /
Cynomolgus Monkey[1] 0.2 mg/kg s.c. 97.2 h 228.9 μg·h/mL 199.0 μg·h/mL 1.8 μg/mL 18 h 75.7 %
Pig[1] 0.16 mg/kg i.v. 101.9 h 142.9 μg·h/mL 140.8 μg·h/mL / / /
Pig[1] 0.16 mg/kg s.c. 129.0 h 174.9 μg·h/mL 170.4 μg·h/mL 1.0 μg/mL 32 h 122.4 %
体内研究
(In Vivo)

TPM003 (3-30 nmol/kg; s.c.; 单次给药) 可在瘦型雄性 C57BL/6J 小鼠中产生剂量依赖性的持续性体重、食物摄入及进食后血糖降低效果[1]。
TPM003 (10 nmol/kg; s.c.; 单次给药) 在高脂饮食诱导的肥胖雄性 C57BL/6J 小鼠中，具有持续的最大减重效果[1]。
TPM003 (10 nmol/kg; s.c.; 每 3 天一次共 21 天) 可在高脂饮食诱导的肥胖雄性 C57BL/6J 小鼠中引发 30% 的体重下降、对食物摄入的强效抑制，以及更出色的肝脏脂质清除作用[1]。
TPM003 (10 nmol/kg; s.c.; 每日一次或每三天一次共 8 周) 在高脂饮食与 CCl4 诱导的小鼠中，诱导显著体重下降和抗纤维化效果[1]。
TPM003 (1.0-3.0 mg/kg; s.c.; 每周两次共 4 周) 可在雄性和雌性 SD 大鼠中诱导食物摄入和体重出现可逆的短暂下降，且无严重不良反应[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (male, 8−10 weeks old)[1]
Dosage: 3 nmol/kg; 10 nmol/kg; 30 nmol/kg
Administration: s.c.; single dose
Result: Induced dose-dependent reductions in body weight, cumulative food intake, and fed blood glucose levels, with maximal effects within 96 hours post dosing.
Sustained body weight reduction effects until day 4 at 30 nmol/kg, when values returned to baseline.
Animal Model: C57BL/6J (male, high-fat diet-induced obesity)[1]
Dosage: 10 nmol/kg
Administration: s.c.; single dose
Result: Induced pronounced reductions in body weight, cumulative food intake, and blood glucose levels within 1−3 days post injection.
Produced a greater maximal weight reduction than retatrutide, with effects sustained without early rebound (unlike tirzepatide, which showed rebound starting at day 4).
Animal Model: C57BL/6J (male, high-fat diet-induced obesity)[1]
Dosage: 10 nmol/kg
Administration: s.c.; every 3 days; 21 days
Result: Achieved approximately 30% body weight reduction over the 21-day treatment period, with cumulative food intake suppressed to levels lower than tirzepatide-treated mice.
Reduced fasting blood glucose, plasma insulin, plasma alanine aminotransferase (ALT), blood triglycerides (TG), blood total cholesterol (TC), liver TG, and liver TC to levels approaching lean control values.
Showed the most substantial clearance of hepatic lipid droplets compared to retatrutide and tirzepatide via Oil Red O staining.
Animal Model: C57BL/6J (male, high-fat diet + carbon tetrachloride-induced NASH)[1]
Dosage: 10 nmol/kg
Administration: s.c.; daily; 8 weeks
Result: Produced a greater reduction in body weight compared to tirzepatide, reduced liver weight to levels approaching lean control values, and significantly decreased hepatic collagen deposition via Masson’s trichrome staining.
Induced significant reductions in key fibrosis markers: α-smooth muscle actin (α-SMA), fibronectin, and collagen type-I α-1 chain (COL1A1), with a significantly greater reduction in α-SMA expression compared to tirzepatide.
Animal Model: C57BL/6J (male, Gubra Amylin NASH diet-induced NASH)[1]
Dosage: 10 nmol/kg
Administration: s.c.; every 3 days; 8 weeks
Result: Induced progressive, sustained body weight loss throughout the 8-week period (with no rebound, unlike retatrutide which showed partial rebound after week 3).
Significantly reduced the NAFLD Activity Score (NAS) compared to both retatrutide and tirzepatide, particularly in steatosis and hepatocellular ballooning components.
Reduced hepatic collagen deposition, COL1A1, and α-SMA expression, indicating robust suppression of hepatic fibrosis and inflammation.
Animal Model: Sprague-Dawley (male, female, 8−10 weeks old)[1]
Dosage: 1.0 mg/kg; 3.0 mg/kg
Administration: s.c.; twice weekly; 4 weeks
Result: Induced transient reductions in food intake and body weight, with occasional emesis and mild diarrhea in a subset of animals; all effects were reversible upon treatment cessation.
No mortality, severe adverse events, overt serum biochemical pathological changes, or abnormal histological findings in key organs (thymus, spleen, mesenteric lymph nodes) were observed.
分子量

5196.91

Formula

C238H370FN51O73S2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TPM003 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TPM003TG062TPM 003TPM-003TG 062TG-062GLP ReceptorGCGRGlucagon ReceptorHEK293 cellsnonalcoholic steatohepatitisobesityGIPRSD ratsC57BL/6J miceinsulin sensitivityGLP-1Rhepatic steatosisInhibitorinhibitorinhibit

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