2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. 4-Methylhistamine

4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki 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.

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4-Methylhistamine

4-Methylhistamine Chemical Structure

CAS No. : 36507-31-0

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Based on 1 publication(s) in Google Scholar

Other Forms of 4-Methylhistamine:

4-Methylhistamine Related Antibodies

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Description

4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki 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[1][2][3][4].

IC50 & Target[1]

H4 receptor

50 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
Sf9 EC50
12400 nM
Compound: 58
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
[PMID: 27007611]
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.

4-Methylhistamine Related Antibodies

Western Blot Analysis[4]

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 models[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: Increased 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 models[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

125.17

Formula

C6H11N3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NCCC1=C(C)N=CN1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 90.00%

SDS (392 KB)

COA (247 KB)

Handling Instructions (2659 KB)
References
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4-Methylhistamine Related Classifications

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Help & FAQs
  • 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:

4-Methylhistamine36507-31-0Histamine ReceptorHistamine 4 receptorH4RA549lung cancerSkin inflammationInhibitorinhibitorinhibit

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