1. GPCR/G Protein
    Immunology/Inflammation
  2. Histamine Receptor
  3. H3R-IN-1 Hydrochloride

H3R-IN-1 Hydrochloride 

Cat. No.: HY-112219A Purity: 95.52%
Handling Instructions

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

For research use only. We do not sell to patients.

H3R-IN-1 Hydrochloride Chemical Structure

H3R-IN-1 Hydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2750 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Description

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

IC50 & Target

Histamine receptor 3[1]

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[1].

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[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6464 mL 13.2321 mL 26.4641 mL
5 mM 0.5293 mL 2.6464 mL 5.2928 mL
10 mM 0.2646 mL 1.3232 mL 2.6464 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

377.87

Formula

C₁₉H₂₄ClN₃O₃

SMILES

[H]Cl.N1(C2CCC2)CCC(CC3=NC(C4=CC=C(OCO5)C5=C4)=NO3)CC1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
H3R-IN-1 Hydrochloride
Cat. No.:
HY-112219A
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H3R-IN-1 Hydrochloride

Cat. No.: HY-112219A