H3R antagonist 1
Based on 1 Customer Validation
H3R antagonist 1 is a histamine receptor 3 (H3R) inverse agonist. H3R antagonist 1 increases the expression levels of myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes. H3R antagonist 1 can be used for the study of multiple sclerosis.
For research use only. We do not sell to patients.
- Purity: 99.21%
- CAS No.: 1448422-61-4
- Formula: C19H23N3O3
- Molecular Weight:341.40
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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All Histamine Receptor Isoforms
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Biological Activity
Histamine receptor 3[1]
H3R antagonist 1 (example 2) promotes oligodendrocyte precursor cell (OPC) differentiation in a dose-dependent manner, at EC50 = 25 nM. Western blot reveals a significant increase in expression levels of two markers of mature oligodendrocytes, myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes after treatment with H3R antagonist 1, which suggests that treatment with H3R antagonist 1 drives more oligodendrocyte precursor cells to differentiate. H3R antagonist 1 increases the Forskolin (HY-15371)-stimulated cAMP level in the primary oligodendrocyte precursor cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1448422-61-4
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Appearance Solid
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Molecular Weight 341.40
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Formula C19H23N3O3
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Color White to off-white
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SMILES
N1(C2CCC2)CCC(CC3=NC(C4=CC=C(OCO5)C5=C4)=NO3)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (292.91 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 (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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Mice[1]
The C57BL/6 mice at age of 8 weeks are fed with powder mouse food mixed freshly with 0.2% Cuprizone (w/w) and receive daily intraperitoneal injection of Rapamycin (10 mg/kg body weight) for 5 weeks to induce demyelination, then animals are allowed to recover (removal of Cuprizone from the diet and Rapamycin injection) and administrated with H3R-IN-1, at 30 mg/kg body weight orally, b.i.d. for an additional 9 days prior to sacrifice. The brain samples are collected for pathologic analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 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 (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 | 2.9291 mL | 14.6456 mL | 29.2912 mL | 73.2279 mL |
| 5 mM | 0.5858 mL | 2.9291 mL | 5.8582 mL | 14.6456 mL | |
| 10 mM | 0.2929 mL | 1.4646 mL | 2.9291 mL | 7.3228 mL | |
| 15 mM | 0.1953 mL | 0.9764 mL | 1.9527 mL | 4.8819 mL | |
| 20 mM | 0.1465 mL | 0.7323 mL | 1.4646 mL | 3.6614 mL | |
| 25 mM | 0.1172 mL | 0.5858 mL | 1.1716 mL | 2.9291 mL | |
| 30 mM | 0.0976 mL | 0.4882 mL | 0.9764 mL | 2.4409 mL | |
| 40 mM | 0.0732 mL | 0.3661 mL | 0.7323 mL | 1.8307 mL | |
| 50 mM | 0.0586 mL | 0.2929 mL | 0.5858 mL | 1.4646 mL | |
| 60 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2205 mL | |
| 80 mM | 0.0366 mL | 0.1831 mL | 0.3661 mL | 0.9153 mL | |
| 100 mM | 0.0293 mL | 0.1465 mL | 0.2929 mL | 0.7323 mL |
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