4-Methylhistamine dihydrochloride

Name: 4-Methylhistamine dihydrochloride
Brand: MedChemExpress
SKU: HY-107560
Rating: 4.5 (1 reviews)

Cat. No.: HY-107560 Purity: 99.35%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

4-Methylhistamine hydrochloride is the dihydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a K_i of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC₅₀ = 7.4). 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation.

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

4-Methylhistamine dihydrochloride Chemical Structure

CAS No. : 36376-47-3

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of 4-Methylhistamine dihydrochloride:

4-Methylhistamine Get quote
4-Methylhistamine hydrochloride Get quote

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

H₄ receptor

In Vitro

4-Methylhistamine (1-10 μM, 12 h) inhibits cell proliferation in A549, H157, H460 and H322 cells^[4].
4-Methylhistamine (1 μM, 12 h) decreases the TGF-β1 mRNA expression in A549 cells^[4].

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

Western Blot Analysis^[1]

Cell Line:	A549, H157, H460 and H322 cells
Concentration:	1 μM
Incubation Time:	12 h
Result:	Increased E-cadherin levels and decreased Vimentin levels.

In Vivo

4-Methylhistamine (30 mg/kg, i.p., twice a day before 2 days prior to stress) modulates the effects of chronic stress on the Th1/Th2 cytokine balance in Balb/c mice^[2].
4-Methylhistamine (20-40 mg/kg, i.p., once a day for 10 days) attenuates Imiquimod (HY-B0180)-induced psoriasis-like skin inflammation in mice^[3].
4-Methylhistamine (100 μmol/kg, i.v., every other day for 33 days) decreases the average tumour volume and prolongs survival in A549 tumor mice^[4].

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

Animal Model:	Balb/c mice with chronic restraint^[2]
Dosage:	30 mg/kg
Administration:	Intraperitoneally injection, twice a day before 2 days prior to stress
Result:	Increase in the CD4⁺ T cells as well as in IFN-γ production. Decreased IL-4 expression. Upregulated expression of IL-1β, IFN-γ and TNF-α mRNA.

Animal Model:	Imiquimod (HY-B0180)-induced psoriasis-like dermatitis mice^[3]
Dosage:	20 and 40 mg/kg
Administration:	Intraperitoneally injection, once a day for 10 days
Result:	Ameliorated the total clinical severity scores. Attenuated the psoriatic phenotypes, including epidermal hyperplasis, hyperkeratosis and lymphocytes infiltration. Led to reductions in the levels of Th1 cytokines (TNF-a, IFN-a, and IL-27). Increased CD4⁺CD25⁺FoxP3⁺ regulatory T (Treg) cells.

Animal Model:	A549 tumor mice^[4]
Dosage:	100 μmol/kg
Administration:	Intravenously injection, every other day for 33 days
Result:	Decreased tumor volume and the proliferation of tumour cells. Prolonged survival of mice. Increased the mRNA expression of E-cadherin and decreased Vimentin levels.

Molecular Weight

198.10

Formula

C₆H₁₃Cl₂N₃

CAS No.

36376-47-3

Appearance

Solid

Color

Off-white to light brown

SMILES

[H]Cl.CC1=C(CCN)NC=N1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°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:

H₂O : 125 mg/mL (631.00 mM; Need ultrasonic)

DMSO : 20 mg/mL (100.96 mM; Need ultrasonic and warming; 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	5.0480 mL	25.2402 mL	50.4803 mL
5 mM	1.0096 mL	5.0480 mL	10.0961 mL
10 mM	0.5048 mL	2.5240 mL	5.0480 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.

Molarity Calculator
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: 99.35%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (251 KB) HNMR (231 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Lim HD, et al. Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21. [Content Brief]

[2]. Ahmad SF, et al. Stimulation of the histamine 4 receptor with 4-methylhistamine modulates the effects of chronic stress on the Th1/Th2 cytokine balance. Immunobiology. 2015 Mar;220(3):341-9. [Content Brief]

[3]. Kim CH, et al. Inhibitory Effect of Imiquimod-Induced Psoriasis-Like Skin Inflammation in Mice by Histamine H4 Receptor Agonist 4-Methylhistamine. Scand J Immunol. 2016 Jun;83(6):409-17. [Content Brief]

[4]. Cai WK, et al. Activation of histamine H4 receptors decreases epithelial-to-mesenchymal transition progress by inhibiting transforming growth factor-β1 signalling pathway in non-small cell lung cancer. Eur J Cancer. 2014 Apr;50(6):1195-206. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / H₂O	1 mM	5.0480 mL	25.2402 mL	50.4803 mL	126.2008 mL
	5 mM	1.0096 mL	5.0480 mL	10.0961 mL	25.2402 mL
	10 mM	0.5048 mL	2.5240 mL	5.0480 mL	12.6201 mL
	15 mM	0.3365 mL	1.6827 mL	3.3654 mL	8.4134 mL
	20 mM	0.2524 mL	1.2620 mL	2.5240 mL	6.3100 mL
	25 mM	0.2019 mL	1.0096 mL	2.0192 mL	5.0480 mL
	30 mM	0.1683 mL	0.8413 mL	1.6827 mL	4.2067 mL
	40 mM	0.1262 mL	0.6310 mL	1.2620 mL	3.1550 mL
	50 mM	0.1010 mL	0.5048 mL	1.0096 mL	2.5240 mL
	60 mM	0.0841 mL	0.4207 mL	0.8413 mL	2.1033 mL
	80 mM	0.0631 mL	0.3155 mL	0.6310 mL	1.5775 mL
	100 mM	0.0505 mL	0.2524 mL	0.5048 mL	1.2620 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.