H4R antagonist 1 manufacturers
- H4R antagonist 1
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- $1520.00 / 25mg
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2024-10-24
- CAS:1429375-54-1
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | H4R antagonist 1 Basic information |
| Product Name: | H4R antagonist 1 | | Synonyms: | H4R antagonist 1;H4R antagonist 1,H-4R antagonist 1;3-Azetidinamine, 1-(8-bromopyrido[2,3-e]tetrazolo[1,5-a]pyrazin-4-yl)-N-methyl- | | CAS: | 1429375-54-1 | | MF: | C11H11BrN8 | | MW: | 335.16 | | EINECS: | | | Product Categories: | | | Mol File: | 1429375-54-1.mol |  |
| | H4R antagonist 1 Chemical Properties |
| density | 2.13±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Solid | | pka | 7.56±0.20(Predicted) | | color | Light yellow to yellow |
| | H4R antagonist 1 Usage And Synthesis |
| 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[1]. 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[1]. H4R antagonist 1 (Compound 48) shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD)[1]. In the [35S]GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC50 of 0.69 μM[1]. | | Uses | 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[1]. | | in vivo | H4R antagonist 1 (Compound 48) shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD)[1].
In the [35S]GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC50 of 0.69 μM[1]. | | IC 50 | Human H4 Receptor: 27 nM (IC50); Mouse H4 Receptor: 290 nM (IC50) | | References | [1]. Ko K, et al. Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis. J Med Chem. 2018 Apr 12;61(7):2949-2961. |
| | H4R antagonist 1 Preparation Products And Raw materials |
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