NGB 2904
Based on 1 Customer Validation
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 189060-98-8
- Formula: C28H29Cl2N3O
- Molecular Weight:494.46
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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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Biological Activity
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D3 Receptor 1.4 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1280 nM
Compound: NGB 2904 (4)
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Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D2 receptor
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D2 receptor
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[PMID: 15916415] |
| CHO | IC50 |
14.4 nM
Compound: NGB 2904 (4)
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Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
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[PMID: 15916415] |
| CHO | IC50 |
5 nM
Compound: NGB 2904 (4)
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Antagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
Antagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor
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[PMID: 15916415] |
| CHO-hD3 | IC50 |
5 nM
Compound: 5 (NGB 2904)
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Compound was tested for stimulation of mitogenesis in CHO.hD3 cells in a dose dependent manner
Compound was tested for stimulation of mitogenesis in CHO.hD3 cells in a dose dependent manner
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[PMID: 9873609] |
| HEK293 | IC50 |
1280 nM
Compound: 3, NGB2904
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Antagonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
Antagonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay
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[PMID: 17672446] |
| HEK293 | IC50 |
14.4 nM
Compound: 3, NGB2904
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Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
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[PMID: 17672446] |
NGB 2904 antagonizes Quinpirole (100 nM)-stimulated mitogenesis, with an IC50 of 5.0 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NGB 2904 (0.026 μg-1 mg/kg; a single s.c. or once daily for 7 d) stimulates spontaneous locomotion in wild-type mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 189060-98-8
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Appearance Solid
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Molecular Weight 494.46
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Formula C28H29Cl2N3O
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Color White to off-white
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SMILES
O=C(C1=CC(CC2=C3C=CC=C2)=C3C=C1)NCCCCN4CCN(C5=CC=CC(Cl)=C5Cl)CC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
Ethanol : 4.55 mg/mL (9.20 mM; ultrasonic and warming and heat to 60°C)
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 (protect from light). 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 (protect from light). 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)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: Corn Oil
Solubility: 5 mg/mL (10.11 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (10.11 mM); Suspended solution; Need ultrasonic
Purity & Documentation
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Data Sheet (271 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Yuan J, et, al. NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2715-8. [Content Brief]
[2]. Xi ZX, et al. The novel dopamine D3 receptor antagonist NGB 2904 inhibits cocaine's rewarding effects and cocaine-induced reinstatement of drug-seeking behavior in rats. Neuropsychopharmacology. 2006;31(7):1393-1405. [Content Brief]
[3]. Pritchard LM, et, al. The dopamine D3 receptor antagonist NGB 2904 increases spontaneous and amphetamine-stimulated locomotion. Pharmacol Biochem Behav. 2007 Apr;86(4):718-26. [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 (protect from light). 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 |
|---|---|---|---|---|---|
| Ethanol | 1 mM | 2.0224 mL | 10.1120 mL | 20.2241 mL | 50.5602 mL |
| 5 mM | 0.4045 mL | 2.0224 mL | 4.0448 mL | 10.1120 mL |
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