2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. H3R antagonist 1

H3R-IN-1 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 antagonist 1 Chemical Structure

H3R antagonist 1 Chemical Structure

CAS No. : 1448422-61-4

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Based on 1 publication(s) in Google Scholar

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H3R antagonist 1 Related Antibodies

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Description

H3R-IN-1 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].

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

H3R antagonist 1 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

341.40

Formula

C19H23N3O3
CAS No.
SMILES

N1(C2CCC2)CCC(CC3=NC(C4=CC=C(OCO5)C5=C4)=NO3)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9291 mL 14.6456 mL 29.2912 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL
View the Complete Stock Solution Preparation Table

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Purity & Documentation
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

Complete Stock Solution Preparation Table

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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H3R antagonist 1 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

H3R antagonist 11448422-61-4Histamine ReceptorInhibitorinhibitorinhibit

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