D3/5-HT receptor modulator-1
Based on 1 Customer Validation
D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile.
For research use only. We do not sell to patients.
- Purity: 99.75%
- CAS No.: 898532-85-9
- Formula: C24H29N3O2
- Molecular Weight:391.51
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
5-HT1A Receptor |
5-HT2A Receptor |
5-HT2C Receptor |
D3 Receptor 4.5 nM (Ki) |
5-HT1A Receptor 11.9 nM (Ki) |
5-HT2A Receptor 15.3 nM (Ki) |
5-HT2C Receptor 206 nM (Ki) |
D2 Receptor 263 nM (Ki) |
D1 Receptor 3290 nM (Ki) |
hERG Channels 930 nM (Ki) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1240 nM
Compound: 5i
|
Antagonist activity at human dopamine D2S receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Antagonist activity at human dopamine D2S receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
[PMID: 19072656] |
| CHO | IC50 |
584 nM
Compound: 5i
|
Antagonist activity at human dopamine D2L receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Antagonist activity at human dopamine D2L receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
[PMID: 19072656] |
| CHO-K1 | IC50 |
143 nM
Compound: 5i
|
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Antagonist activity at human dopamine D3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
|
[PMID: 19072656] |
Chemical Information
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CAS No. 898532-85-9
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Appearance Solid
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Molecular Weight 391.51
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Formula C24H29N3O2
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Color White to off-white
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SMILES
O=C(C1=CC2=CC=CC=C2O1)NCCCCN3CCN(C4=CC=CC(C)=C4)CC3
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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 : 50 mg/mL (127.71 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)
Purity & Documentation
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Data Sheet (269 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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Handling Instructions (2659 KB)
References
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 | 2.5542 mL | 12.7711 mL | 25.5421 mL | 63.8553 mL |
| 5 mM | 0.5108 mL | 2.5542 mL | 5.1084 mL | 12.7711 mL | |
| 10 mM | 0.2554 mL | 1.2771 mL | 2.5542 mL | 6.3855 mL | |
| 15 mM | 0.1703 mL | 0.8514 mL | 1.7028 mL | 4.2570 mL | |
| 20 mM | 0.1277 mL | 0.6386 mL | 1.2771 mL | 3.1928 mL | |
| 25 mM | 0.1022 mL | 0.5108 mL | 1.0217 mL | 2.5542 mL | |
| 30 mM | 0.0851 mL | 0.4257 mL | 0.8514 mL | 2.1285 mL | |
| 40 mM | 0.0639 mL | 0.3193 mL | 0.6386 mL | 1.5964 mL | |
| 50 mM | 0.0511 mL | 0.2554 mL | 0.5108 mL | 1.2771 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4257 mL | 1.0643 mL | |
| 80 mM | 0.0319 mL | 0.1596 mL | 0.3193 mL | 0.7982 mL | |
| 100 mM | 0.0255 mL | 0.1277 mL | 0.2554 mL | 0.6386 mL |