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Art. -Nr.: HY-14364

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A-987306

A-987306 is a potent and oral bioavailable histamine H₄ antagonist, with K_is 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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CAS. Nr.: 1082954-71-9
Formel: C₁₈H₂₅N₅O
Molecular Weight:327.42

Speicherung:

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

Data Sheet (275 KB)

A-987306 Chemical Structure

CAS. Nr.: 1082954-71-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
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Bioz

Biologische Aktivität

Beschreibung

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

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].

MedChemExpress (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 (F_po/iv=26%) with a half-life of 3.7 h and a C_max of 0.30 µM at a T_max of 1.5 h after dosing^[1].

MedChemExpress (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:

F_po/iv=26%, T_1/2=3.7 hours, C_max=0.30 µM, T_max=1.5 hours

Chemical Information

CAS. Nr. 1082954-71-9
Molecular Weight 327.42
Formel C₁₈H₂₅N₅O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia J. Med. Chem., 2008, 51 (22), pp 7094-7098

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Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
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- In Vivo
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A-987306

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

A-987306 Related Classifications

HY-14364 Related Classifications