Pitolisant (oxalate)

CAS Number: 362665-57-4


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Cat No.: 362665-57-4
Biological Description:
Pitolisant oxalate (BF2.649) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
IC50 Value: 0.16 nM (Ki value); 1.5 nM (EC50) [1]
Target: H3 receptor
BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan.
in vitro: BF2.649 behaved as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity approximately 50% higher than that of ciproxifan. Pitolisant in vitro potency was approximately 6 times lower at the rodent receptor [1].
in vivo: In mice, the oral bioavailability coefficient, i.e., the ratio of plasma areas under the curve after oral and i.v. administrations, respectively, was 84%. BF2.649 dose dependently enhanced tele-methylhistamine levels in mouse brain, an index of histaminergic neuron activity, with an ED50 v...

Purity: >98%

Molecular formula: C19H28ClNO5

Molecular Weight: 385.88

Storage Instructions: Two years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

References: for more information, please visit http://www.ncbi.nlm.nih.gov