Enicepatide
Based on 1 Customer Validation
Enicepatide (CT-388) is a cAMP signal-biased dual GLP-1R and GIPR agonist peptide, with an EC50 value of 0.087 nM for GLP-1R cAMP, and an EC50 value of 2.47 nM for GIPR cAMP. Enicepatide activates the cAMP signaling pathway, while recruiting only minimal amounts of β-arrestin-2 at both targets and reducing receptor internalization levels. Enicepatide improves glycemic control, reduces body weight, suppresses appetite, and ameliorates the pathological conditions of metabolic dysfunction-associated steatohepatitis. Enicepatide can be used in the research of obesity, type 2 diabetes, and metabolic dysfunction-associated steatohepatitis.
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- Pureté: 98.16%
- CAS No.: 2869147-44-2
- Formule: C226H345FN48O67
- Masse moléculaire:4825.44
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Stockage:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Enicepatide acts as a cAMP-signaling biased agonist at the human GLP-1 receptor, potently stimulating cAMP production (EC50 = 0.087 nM) while minimally inducing β-arrestin-2 recruitment and receptor internalization in overexpressed mammalian cell lines[1].
Enicepatide acts as a cAMP-signaling biased agonist at the human GIP receptor, stimulating cAMP production (EC50 = 2.47 nM) while inducing only minimal β-arrestin-2 recruitment and no measurable receptor internalization in overexpressed mammalian cell lines[1].
Enicepatide potently enhances glucose-stimulated insulin secretion in EndoC-βH5 human beta cells with an EC50 of 6.4 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Enicepatide (0.15-0.5 mg/kg; s.c.; single dose) dose-dependently increases insulin and C-peptide secretion and lowers blood glucose levels in healthy lean cynomolgus monkeys during an ivGTT[1].
Enicepatide (6 nmol/kg; s.c.; single dose) reduces body weight by ~10% and suppresses food intake in healthy lean mice within 24 hours of a single subcutaneous dose[1].
Enicepatide (2-6 nmol/kg; s.c.; single dose) does not induce significant conditioned taste aversion in healthy lean mice[1].
Enicepatide (6 nmol/kg; s.c.; daily; 21 days) reduces body weight by ~25% and lowers liver weight in diet-induced obese mice[1].
Enicepatide (30 nmol/kg; s.c.; daily; 21 days) reduces body weight by ~20%, suppresses food intake by ~43.5%, and improves glycemic control and metabolic parameters in genetically obese MC4RKO mice[1].
Enicepatide (6 nmol/kg; s.c.; daily; 8 weeks) reduces body weight by ~20% and improves MASH-related pathology, including liver steatosis, hepatocyte ballooning, and liver enzyme levels, in GAN-DIO mice[1].
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)[1]
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Dosage:1 nmol/kg; 2 nmol/kg; 4 nmol/kg
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Administration:s.c.; single dose
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Result:Substantially lowered post-prandial blood glucose levels relative to vehicle controls.
Substantially lowered blood glucose area under the curve (AUC) during the ipGTT relative to vehicle controls.
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Animal Model:C57BL/6J (male)[1]
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Dosage:6 nmol/kg
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Administration:s.c.; single dose
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Result:Lowered body weight by approximately 10% compared with vehicle within 24 hours of administration, with body weight returning toward baseline by 96 hours.
Reduced food intake compared with vehicle controls.
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Animal Model:C57BL/6J (male)[1]
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Dosage:2 nmol/kg; 4 nmol/kg; 6 nmol/kg
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Administration:s.c.; single dose
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Result:Showed minimal taste aversion at doses of up to 6 nmol/kg, unlike semaglutide which showed strong taste-aversion effects at 20 nmol/kg.
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Animal Model:C57BL/6J (male, diet-induced obese, maintained on high-fat diet [60% kcal from fat])[1]
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Dosage:6 nmol/kg
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Administration:s.c.; daily; 21 days
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Result:Reduced body weight by approximately 25% compared with vehicle after 21 days of dosing.
Significantly reduced liver weight compared with vehicle.
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Animal Model:B6.129S4-Mc4rtm1Lowl/J (male, melanocortin receptor 4 knock-out, initially maintained on breeder diet for 5 weeks, then switched to regular chow)[1]
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Dosage:30 nmol/kg
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Administration:s.c.; daily; 21 days
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Result:Reduced body weight from baseline by approximately 20% compared with an 8% increase in vehicle-treated mice.
Decreased accumulated food intake by approximately 41 g (43.5%) compared with vehicle.
Reduced 12-hour fasting glucose levels compared with vehicle controls.
Reduced fasting insulin levels compared with vehicle controls.
Reduced inguinal white adipose tissue (iWAT) weight compared with vehicle controls.
Reduced liver weight compared with vehicle controls.
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Animal Model:C57BL/6NTac (NASH-B6-M, male, maintained on Gubra-Amylin diet [GAN-DIO] starting at 6 weeks of age)[1]
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Dosage:6 nmol/kg
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Administration:s.c.; daily; 8 weeks
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Result:Reduced mean body weight by approximately 20% vs 1% with vehicle after 8 weeks.
Significantly reduced iWAT weight compared with vehicle.
Significantly reduced liver weight compared with vehicle.
Significantly reduced fasting blood glucose compared with vehicle.
Reduced triglyceride levels compared with vehicle.
Reduced circulating alanine aminotransferase (ALT) levels compared with vehicle.
Reduced circulating aspartate aminotransferase (AST) levels compared with vehicle.
Substantially reduced liver lipid accumulation compared with vehicle.
Substantially reduced hepatocyte ballooning compared with vehicle.
Substantially reduced nonalcoholic fatty liver disease activity score (NAS) compared with vehicle.
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Animal Model:cynomolgus monkeys (male, lean)[1]
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Dosage:0.15 mg/kg (31.1 nmol/kg); 0.5 mg/kg (103.6 nmol/kg)
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Administration:s.c.; single dose
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Result:Dose-dependently increased insulin and C-peptide concentrations compared with vehicle during the ivGTT, with biphasic increases characteristic of glucose-stimulated insulin secretion.
Enhanced glucose elimination, demonstrated by significantly lower blood glucose levels compared with vehicle.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2869147-44-2
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Appearance Solid
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Masse moléculaire 4825.44
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Formule C226H345FN48O67
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Color White to off-white
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Synonyms
CT-388
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Sequence
{3'CN,2'F-Phenylisobutyric-βAla}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{Lys((AEEA)2-γGlu-C20 diacid)}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
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Sequence Shortening
{3'CN,2'F-Phenylisobutyric-βAla}-EGTFTSDYSI-{Aib}-LDKIAQ-{Lys((AEEA)2-γGlu-C20 diacid)}-AFVQWLIAGGPSSGAPPPS-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (10.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (306 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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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.2072 mL | 1.0362 mL | 2.0723 mL | 5.1809 mL |
| 5 mM | 0.0414 mL | 0.2072 mL | 0.4145 mL | 1.0362 mL | |
| 10 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.5181 mL |
Enicepatide Related Classifications
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