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H4R antagonist 1

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Catalog No. T11532Cas No. 1429375-54-1

H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.

H4R antagonist 1

H4R antagonist 1

😃Good
Catalog No. T11532Cas No. 1429375-54-1
H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.
Pack SizePriceAvailabilityQuantity
25 mg$1,5206-8 weeks
50 mg$1,9806-8 weeks
100 mg$2,5006-8 weeks
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Product Introduction

Bioactivity
Description
H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.
Targets&IC50
H4 receptor (human):27 nM, H4 receptor (mouse):290 nM
In vitro
The competitive binding assay against a broad panel of GPCRs, ion channels, and transporters at 10 μM shows that H4R antagonist 1 is highly selective for H4R. The inhibitory activity of H4R antagonist 1 against mouse H4R (IC50 = 0.29 μM) is approximately 10 times weaker than that for human H4R.
In vivo
In the GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC50 of 0.69 μM.H4R antagonist 1 shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD).
Chemical Properties
Molecular Weight335.16
FormulaC11H11BrN8
Cas No.1429375-54-1
Relative Density.2.13 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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