GW438014A
Based on 1 Customer Validation
GW438014A is a selective NPY-Y5 receptor competitive antagonist capable of crossing the blood-brain barrier, with IC50 values of 197 nM and 211 nM against human receptors. GW438014A reverses PYY-mediated inhibition of Forskolin (HY-15371)-induced cAMP production, reduces NPY-induced food intake and nocturnal food intake in rodents, decreases body weight gain and fat mass in Zucker rats, and inhibits centrally mediated feeding behavior. GW438014A can be used in research related to obesity and epilepsy.
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- Pureza : 99.98%
- No. CAS: 469861-49-2
- Fòrmula: C23H23N3O4S
- Peso molecular:437.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Help & FAQs
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Actividad biológica
Descripciòn
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NPY Y5 receptor 197-211 nM (IC50) |
In Vitro
GW438014A potently and selectively binds to human Y5 receptors expressed in CHO cell membranes, with a binding IC50 of 211 nM, and shows no affinity for human Y1, Y2, or Y4 receptors at concentrations up to 10,000 nM[1].
GW438014A (10 min) acts as a competitive antagonist of human Y5 receptors in HEC-1B cells, reversing PYY-mediated inhibition of Forskolin (HY-15371)-induced cAMP production with a functional IC50 of 197 nM[1].
GW438014A is a potent, selective competitive antagonist of human Y5 receptors with minimal activity at other NPY receptor subtypes and unrelated targets[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GW438014A (1-10 mg/kg; i.p.; single dose) significantly reduces food intake in 20-hour fasted Sprague-Dawley rats over 3 hours, with minimal effect at lower doses[1].
GW438014A (10 mg/kg; i.p.; single dose) significantly inhibits normal dark-cycle food intake in Sprague-Dawley rats over 16 hours[1].
GW438014A (10 mg/kg; i.p.; single dose) significantly reduces food intake in fasted ob/ob mice, with 50% inhibition persisting for 24 hours[1].
GW438014A (1-10 mg/kg; i.p.; single dose) dose-dependently inhibits overnight dark-cycle food intake in ob/ob mice[1].
GW438014A (10 mg/kg; i.p.; single dose) does not block the anticonvulsant effects of the Y5-preferring agonist AlaAibNPY in kainic acid-induced hippocampal seizures in male C57BL/6 mice[2].
GW438014A (10 mg/kg; i.p.; single dose) significantly accelerates ventral hippocampal rapid kindling acquisition in male Sprague-Dawley rats, reducing the number of stimuli needed to reach stage 2 by 46%, stage 3 by 48%, and stages 4-5 by 25%, while prolonging afterdischarge durations and increasing generalized seizure frequency during stimulation[3].
GW438014A (10 mg/kg; i.p.; twice daily; 4 days) significantly reduces weight gain, food intake, and fat mass in both obese and lean Zucker rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (adult male; hyperphagia model via intracerebroventricular NPY challenge)[1]
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Dosage:3 mg/kg
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Administration:i.p.; single dose
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Result:Produced a statistically significant reduction in NPY-induced cumulative food intake for up to 3 hours post-NPY administration (p < 0.01 for all time points).
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Animal Model:Sprague-Dawley (adult male; hyperphagia model via 20-hour fasting)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Had little or no effect on food intake at 1 and 3 mg/kg.
Produced a marked, statistically significant decrease in cumulative food intake over 3 hours at 10 mg/kg (p < 0.05).
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Animal Model:Sprague-Dawley (adult male; tested during dark cycle feeding period)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Produced a strong, long-lasting, statistically significant inhibitory effect on cumulative food intake throughout the 16-hour dark period (p < 0.01).
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Animal Model:Zucker (13-week-old; obese and lean; obesity model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice daily; 4 days
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Result:Significantly decreased the rate of weight gain in both obese and lean rats compared to vehicle controls (p < 0.05).
Reduced daily food intake by ~20% consistently in both groups.
Significantly reduced fat mass in obese rats (percent change from baseline lower than vehicle controls, p < 0.05) and lean rats (percent change from baseline negative, p < 0.05).
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Animal Model:ob/ob (8-week-old; hyperphagia model via overnight fasting)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Produced a marked, statistically significant inhibition of cumulative food intake from 4 to 7 hours post-dosing (p < 0.01).
Maintained 50% inhibition of food intake at 24 hours post-administration.
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Animal Model:ob/ob (8-week-old; tested during dark cycle feeding period)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Dose-dependently inhibited overnight food intake.
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Animal Model:C57BL/6 (male, ~60 days old, intrahippocampal kainic acid-induced EEG seizures)[2]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Did not alter the ability of the Y5-preferring agonist AlaAibNPY to reduce seizure activity.
Did not affect the 44% reduction in seizure episode number vs. control induced by AlaAibNPY.
Did not affect the 38% reduction in time spent in seizure activity vs. control induced by AlaAibNPY.
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Animal Model:Sprague-Dawley (adult male, 250 g, ventral hippocampal rapid kindling model)[3]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Reduced the number of stimuli needed to reach stage 2 by 46% (p<0.05).
Reduced the number of stimuli needed to reach stage 3 by 48% (p<0.05).
Reduced the number of stimuli needed to reach stages 4-5 by 25% (p<0.01).
Increased the number of generalized clonic seizures (stages 4-5) during the stimulation protocol by 60%.
Prolonged mean primary afterdischarge duration from 24.0 s to 54.0 s (p<0.01).
Prolonged mean secondary afterdischarge duration from 24.0 s to 48.0 s (p<0.01).
Showed a similar number of stages 4-5 seizures as vehicle controls (3.3 vs. 4.4) during the 24-hour re-test session.
Chemical Information
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No. CAS 469861-49-2
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Appearance Solid
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Peso molecular 437.51
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Fòrmula C23H23N3O4S
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Color White to off-white
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SMILES
O=C(C1=CC=CC=C1)NC2=NC3=CC=CC=C3N2CCC4=CC=CC=C4.CS(=O)(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 250 mg/mL (571.42 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. 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. 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)
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Daniels AJ, et al. Food intake inhibition and reduction in body weight gain in lean and obese rodents treated with GW438014A, a potent and selective NPY-Y5 receptor antagonist. Regulatory peptides. 2002 Jun 15;106(1-3):47-54. [Content Brief]
[3]. Benmaamar R, et al. Neuropeptide Y Y5 receptors inhibit kindling acquisition in rats. Regulatory peptides. 2005 Feb 15;125(1-3):79-83. [Content Brief]
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. 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 | 2.2857 mL | 11.4283 mL | 22.8566 mL | 57.1415 mL |
| 5 mM | 0.4571 mL | 2.2857 mL | 4.5713 mL | 11.4283 mL | |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2857 mL | 5.7142 mL | |
| 15 mM | 0.1524 mL | 0.7619 mL | 1.5238 mL | 3.8094 mL | |
| 20 mM | 0.1143 mL | 0.5714 mL | 1.1428 mL | 2.8571 mL | |
| 25 mM | 0.0914 mL | 0.4571 mL | 0.9143 mL | 2.2857 mL | |
| 30 mM | 0.0762 mL | 0.3809 mL | 0.7619 mL | 1.9047 mL | |
| 40 mM | 0.0571 mL | 0.2857 mL | 0.5714 mL | 1.4285 mL | |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4571 mL | 1.1428 mL | |
| 60 mM | 0.0381 mL | 0.1905 mL | 0.3809 mL | 0.9524 mL | |
| 80 mM | 0.0286 mL | 0.1429 mL | 0.2857 mL | 0.7143 mL | |
| 100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.5714 mL |
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