2. GPCR/G Protein
  3. GLP Receptor GCGR
  4. SAR441255

SAR441255 is a GLP-1R/GCGR/GIPR agonist, with human EC50 values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 stimulates receptor activity and drives cAMP accumulation. SAR441255 can be used for the research of type 2 diabetes, obesity.

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SAR441255

SAR441255 Estructura química

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SAR441255 Related Antibodies

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Descripciòn

SAR441255 is a GLP-1R/GCGR/GIPR agonist, with human EC50 values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 stimulates receptor activity and drives cAMP accumulation. SAR441255 can be used for the research of type 2 diabetes, obesity[1][2].

IC50 & Target[1]

GLP-1

1.03 pM (EC50)

In Vitro

SAR441255 (30 min) acts as a potent, balanced agonist of human GLP-1R, GCGR, and GIPR in recombinant HEK293 cells, with EC50 values of 1.03 pM, 1.01 pM, and 0.73 pM respectively[1].
SAR441255 potently activates endogenous human GLP-1R in 1.1B4 pancreatic cells (EC50 27 pM), GCGR in primary human hepatocytes (EC50 2100 pM), and GIPR in human adipocytes (EC50 42 pM)[1].

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

SAR441255 Related Antibodies
Parmacokinetics
Species Dose Route Tmax
Monkey[1] 11 μg/kg s.c. ~2 h
In Vivo

SAR441255 (0.3-30 μg/kg; s.c.; twice daily; 28 days) induces dose-dependent body weight loss, improved glycemic control, and reduced liver injury markers in diet-induced obese mice[1].
SAR441255 (3-11 μg/kg; s.c.; once daily; 42 days) induces significant body weight loss and improves glycemic control in obese, diabetic Macaca fascicularis monkeys over 42 days of treatment[1].
SAR441255 (11 μg/kg; s.c.; single dose) achieves significant in vivo occupancy of GLP-1 receptors in the pancreas and glucagon receptors in the liver of lean cynomolgus monkeys[1].
SAR441255 (3-300 μg/kg; s.c.; once daily; 4 days) causes transient, dose-related increases in heart rate and slight, sustained decreases in systolic blood pressure in lean telemetered cynomolgus monkeys[1].
SAR441255 (0.3-30 μg/kg; s.c.) reduces body weight in a dose-dependent manner[2].

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

Animal Model: C57BL/6NHsd (female, 25-week-old obese, diet-induced obesity model)[1]
Dosage: 0.3 μg/kg; 1 μg/kg; 3 μg/kg; 10 μg/kg; 30 μg/kg
Administration: s.c.; twice daily; 28 days
Result: Produced body weight changes versus baseline of +9.7% (0.3 μg/kg), +6.9% (1 μg/kg), +5.8% (3 μg/kg), -4.8% (10 μg/kg), and -14.1% (30 μg/kg), compared to +11.5% for vehicle controls.
Achieved statistically significant weight reduction at doses of 3 μg/kg or greater versus vehicle.
Lowered nonfasted blood glucose significantly at doses of 1 μg/kg or greater versus vehicle.
Reduced liver weight significantly in the 10 μg/kg (p < 0.001) and 30 μg/kg (p < 0.0001) groups versus vehicle.
Decreased mean serum ALT levels by 73% (10 μg/kg, p < 0.001) and 81% (30 μg/kg, p < 0.0001) versus obese controls.
Reduced mean AST levels by 46% (3 μg/kg, p < 0.001), 55% (10 μg/kg, p < 0.0001), and 58% (30 μg/kg, p < 0.0001) versus obese controls.
Animal Model: Macaca fascicularis (male, obese, diabetic)[1]
Dosage: 3 μg/kg; 5 μg/kg; 8 μg/kg; 11 μg/kg
Administration: s.c.; once daily; 42 days
Result: Produced a mean body weight reduction of -12.6% versus stable weight in vehicle-treated monkeys over 42 days (p < 0.05).
Decreased HbA1c levels by -1.37% (p < 0.05), reaching normoglycemic levels (<5%) at study end.
Lowered fasting plasma glucose and ALT levels significantly versus vehicle.
Showed a non-significant trend toward increased total ketones and 3-hydroxybutyrate levels at study end.
Caused a non-significant increase in FGF21 levels versus vehicle.
Animal Model: Macaca fascicularis (lean)[1]
Dosage: 11 μg/kg
Administration: s.c.; single dose
Result: Produced a mean 40.6% decrease in liver radiotracer binding (indicating GCGR occupancy) versus baseline scans.
Achieved a mean 72.5% decrease in pancreatic radiotracer binding (indicating GLP-1R occupancy) versus baseline scans.
Animal Model: Macaca fascicularis (4 males, 2 females, 3.12-6.10 kg, 37-51 months old, lean, telemetered)[1]
Dosage: 3 μg/kg; 30 μg/kg; 300 μg/kg
Administration: s.c.; once daily; 4 days
Result: Induced a dose-related increase in heart rate on day 1, lasting 10-11 hours for 3 μg/kg and 30 μg/kg doses, and up to 20 hours for 300 μg/kg dose.
Resolved heart rate increase in 3 μg/kg and 30 μg/kg groups by day 4, while it remained slightly elevated in 300 μg/kg group until day 5.
Caused no significant dose-related systolic blood pressure changes on day 1.
Induced a statistically significant, slight (<10 mmHg) decrease in systolic blood pressure lasting over 24 hours across all doses on day 4, with values remaining significantly below vehicle in 30 μg/kg and 300 μg/kg groups on day 5.
Animal Model: Mice (diet-induced obese)[2]
Dosage: 0.3 μg/kg; 1 μg/kg; 3 μg/kg; 10 μg/kg; 30 μg/kg
Administration: s.c.
Result: Produced dose-dependent changes in body weight relative to vehicle-treated mice (which had a +11.5% body weight change): +9.7% at 0.3 μg/kg, +6.9% at 1 μg/kg, +5.8% at 3 μg/kg, -4.8% at 10 μg/kg, and -14.1% at 30 μg/kg.
Lowered non-fasted blood glucose levels significantly in mice treated at doses of ≥1 μg/kg compared with vehicle-treated controls.
Ensayo clínico
Peso molecular

4866.56

Fòrmula

C225H3555N57O63
Appearance

Solid

Color

White to off-white

Sequence Shortening

H-{Aib}-HGTFTSDLSKL-{Lys(γGlu-γGlu-Palm acid)}-EEQRQ-{Aib}-EFIEWLKA-{d-Ala}-GPPS-{Aib}-KPPPK-NH2
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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)

Solvente y solubilidad
In Vitro: 

DMSO : 50 mg/mL (10.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2055 mL 1.0274 mL 2.0548 mL
5 mM 0.0411 mL 0.2055 mL 0.4110 mL
View the 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

V1

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Concentration (final)

C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación
Referencias

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). 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 0.2055 mL 1.0274 mL 2.0548 mL 5.1371 mL
5 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0274 mL
10 mM 0.0205 mL 0.1027 mL 0.2055 mL 0.5137 mL
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SAR441255 Related Classifications

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:

SAR441255SAR 441255SAR-441255GLP ReceptorGCGRGlucagon Receptorprimary human hepatocytes1.1B4 pancreatic cellsGIPRtype 2 diabetesGLP-1RHEK293 cellsdiet-induced obese micehuman adipocytescynomolgus monkeysInhibitorinhibitorinhibit

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Nombre del producto:
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HY-P10031
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