Zenagamtide sodium
Based on 1 Customer Validation
For research use only. We do not sell to patients.
- Purity : 99.96%
- Formula: C343H550N94O116.xNa
- Molecular Weight:7846.60 (free base)
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Storage:
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)
Biological Activity
Description
IC50 & Target
[1]|
GLP-1 |
In Vitro
Zenagamtide (30 min-3 h) sodium potently activates human, mouse, and rat GLP-1R, mouse and rat AMY3 (a)R, and mouse and rat CTR, with EC50 values ranging from 8.4×10-13 M to 7.8×10-11 M[2].
Zenagamtide (30 min) sodium 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.
Parmacokinetics
| 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 |
In Vivo
Zenagamtide (10 nmol/kg; s.c.; single administration) sodium reduces 48-hour cumulative food intake by 50% in normal-weight male Sprague Dawley rats[2].
Zenagamtide (2-10 nmol/kg; s.c.; twice daily; for 21 consecutive days) sodium reduces total food intake by 23-30% and induces vehicle-corrected body weight loss of 15.8-21.3% in a dose-dependent manner in male DIO C57Bl/6J mice[2].
Zenagamtide (1-10 nmol/kg; s.c.; once daily; for 21 days) sodium reduces total energy intake by 47.4% and achieves a vehicle-corrected 18.3% body weight loss in male diet-induced obese (DIO) Sprague Dawley rats while maintaining total energy expenditure[2].
Zenagamtide (1-10 nmol/kg; s.c.; once daily; for 35 days) sodium reduces HOMA-IR by 47% and increases the steady-state glucose infusion rate 3-fold in male diet-induced obese (DIO) Sprague Dawley rats, suggesting improved insulin sensitivity[2].
Zenagamtide (10-30 nmol/kg; s.c.; twice daily; for 12 weeks) sodium reduces plasma liver enzyme levels, improves the MASLD activity score in 55.6%-64.7% of mice, and decreases liver inflammation and fibrosis markers in biopsy-confirmed GAN DIO-MASH male C57BL/6JRj 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.
Chemical Information
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Appearance Solid
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Molecular Weight 7846.60 (free base)
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Formula C343H550N94O116.xNa
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Color White to off-white
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Synonyms
Amycretin sodium; NN 9487 sodium
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Sequence
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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Sequence Shortening
H-Aib-EGTFTSDVSSYLEEQAAREFIAWLVRGR-{Lys(AEEA-AEEA-γGlu-C18 diacid)}-GGGGEASELSTAALGRLSAELHELATLPRTETGSGSP-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Solvent & Solubility
In Vitro:
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)
Purity & Documentation
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Data Sheet (318 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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Handling Instructions (2659 KB)
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Zenagamtide
- Amycretin
- NN 9487
- NN9487
- NN-9487
- Amylin Receptor
- Insulin Receptor
- GLP Receptor
- AMYR
- 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