NCRW0005-F05
Based on 1 Customer Validation
NCRW0005-F05 is a GPR139 antagonist with an IC50 of 147.9 nM against zebrafish GPR139. NCRW0005-F05 blocks agonist-induced GPR139 activity and inhibits intracellular calcium mobilization. NCRW0005-F05 suppresses fear memory consolidation, increases and decreases the peak amplitude of calcium transients, reduces KCl-induced calcium transients, induces thigmotaxis, and decreases locomotor speed after conditioning. NCRW0005-F05 can be used in research related to Parkinson's disease, diabetes, and obesity.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 342779-66-2
- Formula: C16H13F2NO2
- Molecular Weight:289.28
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
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Bioactive Compound Library
HY-L001
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GPCR/G Protein Compound Library
HY-L006
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Neuronal Signaling Compound Library
HY-L013
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Anti-diabetic Compound Library
HY-L040
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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MCE Bioactive Compound Library
HY-L001V
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
Biological Activity
IC50: 0.21 μM (GPR139)[1]
NCRW0005-F05 potently inhibits TC-O 9311 (HY-101777) (Compound 1)-induced calcium mobilization in CHO-K1 cells stably transfected with human GPR139, with an IC50 of 0.21 µM[1].
NCRW0005-F05 is an antagonist of zebrafish GPR139, with an IC50 of 147.9 nM in the dual-luciferase reporter gene assay[2].
NCRW0005-F05 (0.17-1.7 mM) increases the peak amplitude of calcium transients in zebrafish habenular neurons at a concentration of 0.17 mM; it reduces agonist-induced calcium transients at a concentration of 1.7 mM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NCRW0005-F05 (0.2-1.72 mM; immersion; single exposure) induces thigmotaxis (anxiety-like behavior) in zebrafish larvae without impairing their general locomotor parameters[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type (male, >6 months old)[2]
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Dosage:0.1 μg/g BW; 1 μg/g BW; 0.1 μg/g BW (co-treated with 0.1 μg/g BW JNJ-63533054); 1 μg/g BW (co-treated with 0.1 μg/g BW JNJ-63533054)
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Administration:i.c.; single dose
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Result:Showed no significant difference in time spent in the AS-paired preferred compartment between pre- and post-conditioning.
Showed no significant difference in number of entries to the AS-paired compartment between pre- and post-conditioning.
Showed a significant reduction in time spent in the AS-paired preferred compartment between pre- and post-conditioning.
Showed a significant reduction in number of entries to the AS-paired compartment between pre- and post-conditioning.
Showed a significant reduction in time spent in the AS-paired preferred compartment between pre- and post-conditioning.
Showed no significant difference in number of entries to the AS-paired compartment.
Showed no significant difference in time spent in the AS-paired preferred compartment between pre- and post-conditioning.
Showed a significant reduction in number of entries to the AS-paired compartment.
Showed significantly reduced swimming speed during post-conditioning compared to controls.
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Animal Model:larval (7 days post-fertilization)[2]
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Dosage:0.1 mM; 0.2 mM; 0.4 mM; 0.8 mM; 1.72 mM
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Administration:immersion; single exposure
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Result:Showed no significant differences in total swimming distance or total swimming speed compared to vehicle control.
Showed a significant difference in total time spent in the outer zone compared to 0.125% vehicle control.
Showed a significant difference in total time spent in the outer zone compared to 1% vehicle control.
Chemical Information
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CAS No. 342779-66-2
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Appearance Solid
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Molecular Weight 289.28
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Formula C16H13F2NO2
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Color White to off-white
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SMILES
O=C1N(C2=CC=CC=C2)C(C3=CC=C(OC)C=C3)C1(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (345.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang J, et al. High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139. Acta pharmacologica Sinica. 2015 Jul;36(7):874-8. [Content Brief]
[2]. Roy N, et al. GPR139 agonist and antagonist differentially regulate retrieval and consolidation of fear memory in the zebrafish. Frontiers in neuroscience. 2024;18:1461148. [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 | 3.4569 mL | 17.2843 mL | 34.5686 mL | 86.4215 mL |
| 5 mM | 0.6914 mL | 3.4569 mL | 6.9137 mL | 17.2843 mL | |
| 10 mM | 0.3457 mL | 1.7284 mL | 3.4569 mL | 8.6421 mL | |
| 15 mM | 0.2305 mL | 1.1523 mL | 2.3046 mL | 5.7614 mL | |
| 20 mM | 0.1728 mL | 0.8642 mL | 1.7284 mL | 4.3211 mL | |
| 25 mM | 0.1383 mL | 0.6914 mL | 1.3827 mL | 3.4569 mL | |
| 30 mM | 0.1152 mL | 0.5761 mL | 1.1523 mL | 2.8807 mL | |
| 40 mM | 0.0864 mL | 0.4321 mL | 0.8642 mL | 2.1605 mL | |
| 50 mM | 0.0691 mL | 0.3457 mL | 0.6914 mL | 1.7284 mL | |
| 60 mM | 0.0576 mL | 0.2881 mL | 0.5761 mL | 1.4404 mL | |
| 80 mM | 0.0432 mL | 0.2161 mL | 0.4321 mL | 1.0803 mL | |
| 100 mM | 0.0346 mL | 0.1728 mL | 0.3457 mL | 0.8642 mL |
NCRW0005-F05 Related Classifications
HY-128057 Related Classifications
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