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H3R-IN-1 Hydrochloride

Catalog No. T11531   CAS 2319790-07-1

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

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H3R-IN-1 Hydrochloride Chemical Structure
H3R-IN-1 Hydrochloride, CAS 2319790-07-1
Pack Size Availability Price/USD Quantity
25 mg 10-14 weeks $ 1,110.00
50 mg 10-14 weeks $ 1,450.00
100 mg 10-14 weeks $ 2,280.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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 ability of H3R-IN-1 to enhance remyelination in vivo is determined using the Cuprizone/Rapamycin-induced demyelination model. Mice are treated with Cuprizone diet combined with intraperitoneal injections of Rapamycin for 5 weeks followed by 9 days of compound administration. Cuprizone diet plus intraperitoneal injections of Rapamycin induced severe demyelination in both corpus callosum and cortex and treatment with H3R-IN-1 (30 mg/kg, 9 days) significantly increases density of myelin specific Black-gold II staining in the lesion of corpus callosum and cortex in forebrain, compared to vehicle control group [1].
Molecular Weight 377.87
Formula C19H24ClN3O3
CAS No. 2319790-07-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (66.16 mM), Sonification is recommended.

TargetMolReferences and Literature

1. WANG, Rong, et al. THERAPEUTIC USES. WO2013107336A1.

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H3 receptor antagonist 1 Betahistine mesylate Acrivastine Clemastine Maprotiline hydrochloride Tecastemizole Psoralenoside Mianserin hydrochloride

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Keywords

H3R-IN-1 Hydrochloride 2319790-07-1 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor H3RIN1 Hydrochloride H3R IN 1 Hydrochloride H-3R-IN-1 Hydrochloride inhibitor inhibit

 

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