A-987306
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.
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- No. CAS: 1082954-71-9
- Fòrmula: C18H25N5O
- Peso molecular:327.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
A-987306 has potent functional antagonism in vitro at human, rat, and mouse H4 receptors in cell-based FLIPR assays[1].
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)[1].
A-987306 shows lower selectivity for H4R in the rat (only 4-fold selective for the rat H4R over the rat H3R) in FLIPR[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:98.23 μg/kg , 327.42 μg/kg, 982.26 μg/kg, 9.82 mg/kg (Pharmacokinetic Analysis)
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Administration:Intraperitoneal injection
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Result:Fpo/iv=26%, T1/2=3.7 hours, Cmax=0.30 µM, Tmax=1.5 hours
Chemical Information
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No. CAS 1082954-71-9
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Peso molecular 327.42
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Fòrmula C18H25N5O
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SMILES
NC1=NC(N2CCNCC2)=C3CCC(O[C@]4([H])[C@@]5([H])CCCC4)=C5C3=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A-987306 Related Classifications
HY-14364 Related Classifications
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