Description
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.
Product information
CAS Number: 1429375-54-1
Molecular Weight: 335.16
Formula: C11H11BrN8
Chemical Name: 1-{12-bromo-2,3,4,5,8,10-hexaazatricyclo[7.4.0.0²,⁶]trideca-1(9),3,5,7,10,12-hexaen-7-yl}-N-methylazetidin-3-amine
Smiles: CNC1CN(C1)C1=NC2N=CC(Br)=CC=2N2N=NN=C21
InChiKey: ICGICUHMULRYIQ-UHFFFAOYSA-N
InChi: InChI=1S/C11H11BrN8/c1-13-7-4-19(5-7)10-11-16-17-18-20(11)8-2-6(12)3-14-9(8)15-10/h2-3,7,13H,4-5H2,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
The competitive binding assay against a wider panel of GPCR, ion channel, and transporters at the concentration of 10 μM reveals that H4R antagonist 1 (Compound 48) is highly selective for H4R. The inhibitory activity of H4R antagonist 1 against mouse H4R (IC50=0.29 μM) is about 10 times weaker than that for human H4R.
In Vivo:
H4R antagonist 1 (Compound 48) shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD). In the [35S]GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC50 of 0.69 μM.
Products are for research use only. Not for human use.
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