H4R antagonist 1

Name: H4R antagonist 1
Brand: TargetMol
SKU: T11532
Rating: 4.5 (1 reviews)

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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

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Catalog No. T11532Cas No. 1429375-54-1

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	6-8 weeks	6-8 weeks
50 mg	$1,980	6-8 weeks	6-8 weeks
100 mg	$2,500	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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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 (mouse):290 nM, H4 receptor (human):27 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 Weight	335.16
Formula	C₁₁H₁₁BrN₈
Cas No.	1429375-54-1
Relative Density.	2.13 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

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