H4R antagonist 1
- CAS No.
- 1429375-54-1
- Chemical 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-
- CBNumber:
- CB44844853
- Molecular Formula:
- C11H11BrN8
- Molecular Weight:
- 335.16
- MDL Number:
- MFCD31813646
- MOL File:
- 1429375-54-1.mol
H4R antagonist 1 Chemical Properties,Uses,Production
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].
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
Raw materials
Preparation Products
H4R antagonist 1 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9730 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 9946 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24023 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| Aladdin Scientific | 58 |
| Fan De(Beijing) Biotechnology Co., Ltd. | 58 |
| DC Chemicals | 58 |
| cjbscvictory | 58 |
| TargetMol Chemicals Inc. | 58 |