H3R antagonist 1 hydrochloride

Name: H3R antagonist 1 hydrochloride
Brand: MedChemExpress
SKU: HY-112219A
Rating: 4.5 (1 reviews)

Cat. No.: HY-112219A Purity: 99.10%: FAQs
Data Sheet SDS COA Handling Instructions

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H3R antagonist 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 antagonist 1 hydrochloride Chemical Structure

CAS No. : 2319790-07-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 385	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 385	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 550	Get quote	Estimated Time of Arrival: December 31
25 mg	USD 1100	Get quote	Estimated Time of Arrival: December 31
50 mg	USD 1750	Get quote	Estimated Time of Arrival: December 31
100 mg	USD 2750	Get quote	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of H3R antagonist 1 hydrochloride:

H3R antagonist 1 Get quote

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•Related Small Molecules:

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

H₃ receptor

In Vitro

Treatment with H3R antagonist 1 hydrochloride, 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 antagonist 1 hydrochloride, which suggests that treatment with H3R antagonist 1 hydrochloride drives more OPCs to differentiate. H3R antagonist 1 hydrochloride 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.

In Vivo

The ability of H3R antagonist 1 hydrochloride-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 antagonist 1 hydrochloride (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

377.87

Formula

C₁₉H₂₄ClN₃O₃

CAS No.

2319790-07-1

Appearance

Solid

Color

White to off-white

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.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (66.16 mM; Need warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (66.16 mM; Need ultrasonic)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.10%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (253 KB) HNMR (370 KB) RP-HPLC (267 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

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

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

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.6464 mL	13.2321 mL	26.4641 mL	66.1603 mL
	5 mM	0.5293 mL	2.6464 mL	5.2928 mL	13.2321 mL
	10 mM	0.2646 mL	1.3232 mL	2.6464 mL	6.6160 mL
	15 mM	0.1764 mL	0.8821 mL	1.7643 mL	4.4107 mL
	20 mM	0.1323 mL	0.6616 mL	1.3232 mL	3.3080 mL
	25 mM	0.1059 mL	0.5293 mL	1.0586 mL	2.6464 mL
	30 mM	0.0882 mL	0.4411 mL	0.8821 mL	2.2053 mL
	40 mM	0.0662 mL	0.3308 mL	0.6616 mL	1.6540 mL
	50 mM	0.0529 mL	0.2646 mL	0.5293 mL	1.3232 mL
	60 mM	0.0441 mL	0.2205 mL	0.4411 mL	1.1027 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.