1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. A-987306

A-987306 

Cat. No.: HY-14364
Handling Instructions

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.

For research use only. We do not sell to patients.

A-987306 Chemical Structure

A-987306 Chemical Structure

CAS No. : 1082954-71-9

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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[1].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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)[1].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice[1]
Dosage: 98.23 μg/kg , 327.42 μg/kg, 982.26 μg/kg, 9.82 mg/kg (Pharmacokinetic Analysis)
Administration: Intraperitoneal injection
Result: Fpo/iv=26%, T1/2=3.7 hours, Cmax=0.30 µM, Tmax=1.5 hours
Molecular Weight

327.42

Formula

C₁₈H₂₅N₅O

CAS No.

1082954-71-9

SMILES

NC1=NC(N2CCNCC2)=C3CCC(O[[email protected]]4([H])[[email protected]@]5([H])CCCC4)=C5C3=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

A-987306A987306A 987306Histamine Receptorhistamineanti-inflammatoryH4H3receptorInhibitorinhibitorinhibit

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A-987306
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HY-14364
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