Zenagamtide sodium
Based on 1 Customer Validation
Zenagamtide (Amycretin; NN 9487) sodium is an orally active, blood-brain barrier permeable triple agonist that targets GLP-1, amylin (Amylin Receptor) and calcitonin receptor (Calcitonin Receptor). Zenagamtide sodium is a single peptide consisting of 68 amino acids that can target brain regions regulating food intake, significantly suppress appetite and reduce energy intake. Therefore, Zenagamtide sodium improves body weight, waist circumference, glycated hemoglobin and lipid profile, and also alleviates the histological features of metabolic dysfunction-associated steatotic liver disease (MASLD) and enhances insulin sensitivity. Zenagamtide sodium may cause transient increases in heart rate and fluctuations in serum calcium levels, but it is an important compound for the study of overweight, obesity, insulin resistance and related metabolic diseases.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.96%
- 分子式: C343H550N94O116.xNa
- 分子量:7846.60 (free base)
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
GLP-1[1]
Zenagamtide sodium activates GLP-1, amylin and calcitonin receptors in cellular systems of humans, mice and rats[1].
Zenagamtide sodium (10-fold to 3-fold serial dilution; 30 min-3 h) potently activates human, mouse and rat GLP-1R, mouse and rat AMY3 (a)R, as well as mouse and rat CTR, with EC50 values ranging from 8.4×10-13 M to 7.8×10-11 M[2].
Zenagamtide sodium (10-fold serial dilution; 30 min) potently activates human AMY1 (a)R, AMY2 (a)R, AMY3 (a)R, and CTR (a), with EC50 values ranging from 1.30×10-12 M to 1.72×10-11 M[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | AUC0-∞ | T1/2 | C0 | CL | Vz |
|---|---|---|---|---|---|---|---|---|---|
| Mice[2] | 0.08 (10 nmol/kg) mg/kg | s.c. | 37.7 nM | 2.00 h | 309 ng·h/mL | 3.65 h | / | / | / |
| Rat[2] | 0.012 (1.5 nmol/kg) mg/kg | i.v. | / | / | 94.4 ng·h/mL | 5.92 h | 19.2 nM | 0.0160 L/h/kg | 0.137 L/kg |
| Pig[2] | 0.016 (1.5 nmol/kg) mg/kg | i.v. | / | / | 1510 ng·h/mL | 54.1 h | 44.7 nM | 0.00122 L/h/kg | 0.0956 L/kg |
Zenagamtide (sodium) (10 nmol/kg; s.c.; single dose) reduces 48-hour cumulative food intake by 50% in normal weight male Sprague Dawley rats[2].
Zenagamtide (sodium) (2-10 nmol/kg; s.c.; twice daily; 21 days) reduces total food intake by 23-30% and induces vehicle-adjusted body weight loss of 15.8-21.3% in a dose-dependent manner in male DIO C57Bl/6J mice[2].
Zenagamtide (sodium) (1→3→10 nmol/kg; s.c.; once daily; 21 days) reduces total energy intake by 47.4% and induces 18.3% vehicle-adjusted body weight loss while maintaining total energy expenditure in male DIO Sprague Dawley rats[2].
Zenagamtide (sodium) (1→3→10 nmol/kg; s.c.; once daily; 35 days) reduces HOMA-IR by 47% and increases steady-state glucose infusion rate three-fold, indicating improved insulin sensitivity, in male DIO Sprague Dawley rats[2].
Zenagamtide (sodium) (10-30 nmol/kg; s.c.; twice daily; 12 weeks) reduces plasma liver enzyme levels, improves MASLD activity scores in 55.6-64.7% of mice, and reduces liver inflammation and fibrosis markers in biopsy-confirmed GAN DIO-MASH male C57BL/6JRj mice[2].
Fluorescently labelled Zenagamtide (sodium) (100 nmol/kg; i.v.; single dose) reaches key brain regions involved in energy intake regulation, including circumventricular organs and hypothalamic/hindbrain regions, in male C57BL/6J mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6J (male, 25 weeks old, 39-56 g, diet-induced obese)[2]
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Dosage:2 nmol/kg; 10 nmol/kg
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Administration:s.c.; twice daily; 21 days
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Result:Reduced total 21-day food intake by 23% with 2 nmol/kg and 30% with 10 nmol/kg.
Induced vehicle-adjusted body weight loss of 15.8% with 2 nmol/kg and 21.3% with 10 nmol/kg, with a significant difference between the two target reagent doses.
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Animal Model:Sprague Dawley (male, ~750 g, diet-induced obese)[2]
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Dosage:1 nmol/kg (day 1); 3 nmol/kg (day 2); 10 nmol/kg (days 3-21)
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Administration:s.c.; once daily; 21 days
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Result:Induced 18.3% vehicle-adjusted body weight loss after 21 days.
Reduced total energy intake by 47.4% compared to vehicle control.
Showed no significant difference in total energy expenditure compared to vehicle groups, while the calorie-restricted weight-matched group had 13.6% lower total energy expenditure than the target reagent group.
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Animal Model:Sprague Dawley (male, diet-induced obese)[2]
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Dosage:1 nmol/kg (day 1); 3 nmol/kg (day 2); 10 nmol/kg (days 3-35)
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Administration:s.c.; once daily; 35 days
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Result:Reduced baseline fasting blood glucose by 7% (vehicle: 121.1 ± 3.0 mg/dL vs.
target reagent: 112 ± 2.1 mg/dL; p < 0.05).
Reduced baseline fasting plasma insulin by 42% (vehicle: 77.0 ± 6.7 µU/mL vs.
target reagent: 44.8 ± 4.0 µU/mL; p < 0.001).
Reduced HOMA-IR by 47% (vehicle: 23.4 ± 2.3 vs.
target reagent: 12.5 ± 1.2; p < 0.001).
Required a three-fold higher glucose infusion rate to maintain euglycaemia during clamp (average steady-state GIR: vehicle: 5.53 ± 1.17 mg/kg/min vs.
target reagent: 16.4 ± 2.10 mg/kg/min; p < 0.001).
Increased tracer-determined glucose uptake by 37% compared to vehicle control (vehicle: 15.7 ± 1.51 mg/kg/min vs.
target reagent: 24.8 ± 1.33 mg/kg/min; p < 0.001), while hepatic glucose production did not differ between groups.
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Animal Model:C57BL/6JRj (male, Gubra-Amylin NASH diet-induced obese metabolic dysfunction-associated steatotic liver disease, fibrosis stage F2-3, steatosis score 3, inflammation score ≥2)[2]
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Dosage:10 nmol/kg (titrated: 0.5→1→2→6→10 nmol/kg); 30 nmol/kg (titrated: 0.5→1→2→6→12→30 nmol/kg)
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Administration:s.c.; twice daily; 12 weeks
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Result:Significantly reduced plasma alanine transaminase (ALT) and aspartate transaminase (AST) levels with both doses (p < 0.001 vs.
vehicle).
Achieved ≥2-point improvement in MASLD activity score in 55.6% of mice treated with 10 nmol/kg and 64.7% treated with 30 nmol/kg (p < 0.001 vs.
vehicle, which had 0% improvement).
Significantly reduced liver galectin-3 staining (inflammation marker) with both doses (p < 0.05 for 10 nmol/kg, p < 0.01 for 30 nmol/kg vs.
vehicle).
Significantly reduced liver α-smooth muscle actin staining (fibrosis marker) with both doses (p < 0.001 vs.
vehicle).
Reduced hepatocytes with lipid droplets to 42.2% with 10 nmol/kg and 29.4% with 30 nmol/kg (p < 0.001 vs.
vehicle's 77.9%).
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Animal Model:C57BL/6J (male, 25 g)[2]
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Dosage:100 nmol/kg
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Administration:i.v.; single dose
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Result:Detected fluorescent signal in circumventricular organs (area postrema, median eminence, vascular organ of the lamina terminalis, subfornical organ) and blood-brain barrier-protected regions (arcuate hypothalamic nucleus, nucleus of the solitary tract, dorsal motor nucleus of the vagus nerve) at 2 and 6 hours post-dose.
Showed highest signal intensity in circumventricular organs at 2 hours post-dose.
化学情報
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性状 Solid
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分子量 7846.60 (free base)
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分子式 C343H550N94O116.xNa
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Color White to off-white
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別名
Amycretin sodium; NN 9487 sodium
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配列
His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Glu-Gln-Ala-Ala-Arg-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-{Lys(AEEA-AEEA-γGlu-C18 diacid)}-Gly-Gly-Gly-Gly-Glu-Ala-Ser-Glu-Leu-Ser-Thr-Ala-Ala-Leu-Gly-Arg-Leu-Ser-Ala-Glu-Leu-His-Glu-Leu-Ala-Thr-Leu-Pro-Arg-Thr-Glu-Thr-Gly-Ser-Gly-Ser-Pro-NH2
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シーケンスの短縮
H-Aib-EGTFTSDVSSYLEEQAAREFIAWLVRGR-{Lys(AEEA-AEEA-γGlu-C18 diacid)}-GGGGEASELSTAALGRLSAELHELATLPRTETGSGSP-NH2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
H2O : 10 mg/mL (Need ultrasonic)
DMSO : 2 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
純度とドキュメンテーション
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データシート (317 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Kuhre RE, et al. The effect of amycretin, a unimolecular glucagon-like peptide-1 and amylin receptor agonist, on body weight and metabolic dysfunction in mice and rats. EBioMedicine. 2025;118:105862. [Content Brief]
[3]. Gasiorek A, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of the first-in-class GLP-1 and amylin receptor agonist, amycretin: a first-in-human, phase 1, double-blind, randomised, placebo-controlled trial. Lancet. 2025;406(10499):135-148. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Zenagamtide sodium 関連分類
HY-P11274A 関連分類
Powered by Bioz
- Zenagamtide
- Amycretin
- NN 9487
- NN9487
- NN-9487
- Amylin Receptor
- Insulin Receptor
- GCGR
- amylin receptor
- metabolic dysfunction-associated steatotic liver disease
- mouse GLP-1R
- Sprague Dawley rats
- hypothalamic/hindbrain regions
- GLP-1 receptor
- rat GLP-1R
- human GLP-1R
- calcitonin receptor
- C57Bl/6J mice
- Inhibitor
- inhibitor
- inhibit