Description
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model.
Product information
CAS Number: 1082954-71-9
Molecular Weight: 327.42
Formula: C18H25N5O
Chemical Name: (12R,17R)-6-(piperazin-1-yl)-11-oxa-3,5-diazatetracyclo[8.7.0.0²,⁷.0¹²,¹⁷]heptadeca-1(10),2,4,6-tetraen-4-amine
Smiles: NC1=NC(=C2CCC3O[C@@H]4CCCC[C@@H]4C=3C2=N1)N1CCNCC1
InChiKey: DJKJVWJQAVGLHJ-WCQYABFASA-N
InChi: InChI=1S/C18H25N5O/c19-18-21-16-12(17(22-18)23-9-7-20-8-10-23)5-6-14-15(16)11-3-1-2-4-13(11)24-14/h11,13,20H,1-10H2,(H2,19,21,22)/t11-,13+/m0/s1
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:
A-987306 has potent functional antagonism in vitro at human, rat, and mouse H4 receptors in cell-based FLIPR assays. A-987306 is 620-fold, >1600-fold, and 162-fold selective for the human H4R over the human H1, H2 , and H3 receptors in cell-based Ca2+-flux functional assay (FLIPR). A-987306 shows lower selectivity for H4R in the rat (only 4-fold selective for the rat H4R over the rat H3R) in FLIPR.
In Vivo:
A-987306 (98.23 μg/kg-9.82 mg/kg; i.p.) is found to reduce scratching induced by the histamine H4 agonist clobenpropit (HY-101198). A-987306 (10 mg/kg; p.o.) has a moderate fractional oral bioavailability (Fpo/iv=26%) with a half-life of 3.7 h and a Cmax of 0.30 µM at a Tmax of 1.5 h after dosing.
Products are for research use only. Not for human use.
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