H4 Receptor antagonist 1

• CAT Number: I019666
• CAS Number: 848217-00-5
• Molecular Formula: C16H17ClN4O
• Molecular Weight: 316.79
• Purity: ≥95%
• Synonyms: 8-chloro-2-methyl-4-(4-methylpiperazin-1-yl)-[1]benzofuro[3,2-d]pyrimidine
• InChI: InChI=1S/C16H17ClN4O/c1-10-18-14-12-9-11(17)3-4-13(12)22-15(14)16(19-10)21-7-5-20(2)6-8-21/h3-4,9H,5-8H2,1-2H3
• InChIKey: GUJLUPNSRRNJKP-UHFFFAOYSA-N
• SMILES: CC1=NC2=C(C(=N1)N3CCN(CC3)C)OC4=C2C=C(C=C4)Cl

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM[1].
H4 Receptor antagonist 1 indicates that metabolic stability in rat microsomes is very low with only 1% parent compound remaining after 10 min incubation[1].

Reference

[1]. Cramp S, et al. Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2516-9.
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