H3R-IN-1 Hydrochloride is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.

Product information

CAS Number: 2319790-07-1

Molecular Weight: 377.87

Formula: C19H24ClN3O3

Chemical Name: 3-(benzo[d][1, 3]dioxol-5-yl)-5-((1-cyclobutylpiperidin-4-yl)methyl)-1, 2, 4-oxadiazole hydrochloride

Smiles: Cl.C(C1CCN(CC1)C1CCC1)C1=NC(=NO1)C1C=C2OCOC2=CC=1

InChiKey: AUFJPTAYJFKWNF-UHFFFAOYSA-N

InChi: InChI=1S/C19H23N3O3.ClH/c1-2-15(3-1)22-8-6-13(7-9-22)10-18-20-19(21-25-18)14-4-5-16-17(11-14)24-12-23-16;/h4-5,11,13,15H,1-3,6-10,12H2;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 25 mg/mL (66.16 mM; Need warming).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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 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-IN-1, which suggests 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.

In Vivo:

The ability of H3R-IN-1 to enhance in vivo remyelination is determined with 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.

Products are for research use only. Not for human use.