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H3R-IN-1 Hydrochloride is an inverse agonist of histamine receptor 3( H3R ) .

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $1,980 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,500 | 6-8 weeks | 6-8 weeks |
| Description | H3R-IN-1 Hydrochloride is an inverse agonist of histamine receptor 3( H3R ) . |
| In vitro | Treatment with H3R-IN-1, which is a H3R inverse agonist, promotes oligodendrocyte precursor cell (OPC) differentiation in a dose-dependent manner, at EC 50 =25 nM. Western blot shows 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-IN-1, which reveals that treatment with H3R-IN-1 drives more OPCs to differentiate. H3R-IN-1 increases the Forskolin-stimulated cAMP level in the primary oligodendrocyte precursor cells in a dose-dependent manner [1]. |
| In vivo | The efficacy of H3R-IN-1 in promoting remyelination in vivo is assessed using the Cuprizone/Rapamycin-induced demyelination model. Mice receive a Cuprizone diet and intraperitoneal Rapamycin injections for 5 weeks, followed by 9 days of H3R-IN-1 treatment (30 mg/kg). Cuprizone and Rapamycin induced severe demyelination in the corpus callosum and cortex, and H3R-IN-1 administration significantly increased myelin-specific Black-gold II staining density in the lesions compared to the vehicle control group [1]. |
| Molecular Weight | 377.86 |
| Formula | C19H24ClN3O3 |
| Cas No. | 2319790-07-1 |
| Smiles | [H]Cl.N1(C2CCC2)CCC(CC3=NC(C4=CC=C(OCO5)C5=C4)=NO3)CC1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 25 mg/mL (66.16 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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