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Pitolisant - ≥98%, high purity , Histamine H3 receptor inverse agonist, CAS No.362665-56-3, Histamine H3 receptor inverse agonist

  • Moligand™
  • ≥98%
Item Number
P126755
Grouped product items
SKUSizeAvailabilityPrice Qty
P126755-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$78.90
P126755-25mg
25mg
In stock
$147.90
P126755-50mg
50mg
In stock
$246.90
P126755-100mg
100mg
In stock
$395.90

Basic Description

SynonymsPitolisant|362665-56-3|TIPROLISANT|wakix|1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine|BF2.649|HBS-101|1-{3-[3-(4-chlorophenyl)propoxy]propyl}piperidine|UNII-4BC83L4PIY|4BC83L4PIY|1-(3-(3-(4-Chlorophenyl)propoxy)propyl)piperidine|Piperidine, 1-[3-[3-(
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological Mechanisms

Description:
IC50 Value: 0.16 nM(Ki value); 1.5 nM(EC50) [1]
Pitolisant (BF2.649) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor. BF2.649 behaved as a competitive antagonist w

Shipped InNormal
GradeMoligand™
Action TypeANTAGONIST, INVERSE AGONIST
Mechanism of actionHistamine H3 receptor inverse agonist
Note卖完停产,不再备货
Product Description

Pitolisant (BF2.649) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).

Product Properties

ALogP4.3

Associated Targets

CNR1 Tclin Cannabinoid receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD1 Tclin D(1A) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD2 Tclin D(2) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ESR1 Tclin Estrogen receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GPATCH2 Tdark G patch domain-containing protein 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NR3C1 Tclin Glucocorticoid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AVPR1A Tclin Vasopressin V1a receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM3 Tclin Muscarinic acetylcholine receptor M3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2B Tclin Alpha-2B adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA2A Tclin Adenosine receptor A2a 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ACHE Tclin Acetylcholinesterase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AR Tclin Androgen receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2C Tclin 5-hydroxytryptamine receptor 2C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA1 Tclin Adenosine receptor A1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA3 Tchem Adenosine receptor A3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR3A Tclin 5-hydroxytryptamine receptor 3A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TBXA2R Tclin Thromboxane A2 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BCHE Tclin Cholinesterase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EDNRA Tclin Endothelin-1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRD1 Tclin Delta-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRK1 Tclin Kappa-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRM1 Tclin Mu-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MLNR Tchem Motilin receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine
INCHI InChI=1S/C17H26ClNO/c18-17-9-7-16(8-10-17)6-4-14-20-15-5-13-19-11-2-1-3-12-19/h7-10H,1-6,11-15H2
InChi Key NNACHAUCXXVJSP-UHFFFAOYSA-N
Canonical SMILES C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl
Isomeric SMILES C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl
PubChem CID 9948102
Molecular Weight 295.85

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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4 results found

Lot NumberCertificate TypeDateItem
G1520086Certificate of AnalysisFeb 03, 2023 P126755
A2213424Certificate of AnalysisFeb 12, 2022 P126755
A2214123Certificate of AnalysisFeb 12, 2022 P126755
A2214124Certificate of AnalysisFeb 12, 2022 P126755

Chemical and Physical Properties

SolubilityDMSO

Related Documents

References

1. Ligneau X, Perrin D, Landais L, Camelin JC, Calmels TP, Berrebi-Bertrand I, Lecomte JM, Parmentier R, Anaclet C, Lin JS et al..  (2007)  BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology..  J Pharmacol Exp Ther,  320  (1): (365-75).  [PMID:17005916]
2. Lin JS, Dauvilliers Y, Arnulf I, Bastuji H, Anaclet C, Parmentier R, Kocher L, Yanagisawa M, Lehert P, Ligneau X et al..  (2008)  An inverse agonist of the histamine H(3) receptor improves wakefulness in narcolepsy: studies in orexin-/- mice and patients..  Neurobiol Dis,  30  (1): (74-83).  [PMID:18295497]
3. Celanire S, Wijtmans M, Talaga P, Leurs R, de Esch IJ.  (2005)  Keynote review: histamine H3 receptor antagonists reach out for the clinic..  Drug Discov Today,  10  (23-24): (1613-27).  [PMID:16376822]
4. Stocking EM, Letavic MA.  (2008)  Histamine H3 antagonists as wake-promoting and pro-cognitive agents..  Curr Top Med Chem,  (11): (988-1002).  [PMID:18673168]
5. Pierson PD, Fettes A, Freichel C, Gatti-McArthur S, Hertel C, Huwyler J, Mohr P, Nakagawa T, Nettekoven M, Plancher JM et al..  (2009)  5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity..  J Med Chem,  52  (13): (3855-68).  [PMID:19456097]
6. Ligneau X, Landais L, Perrin D, Piriou J, Uguen M, Denis E, Robert P, Parmentier R, Anaclet C, Lin JS et al..  (2007)  Brain histamine and schizophrenia: potential therapeutic applications of H3-receptor inverse agonists studied with BF2.649..  Biochem Pharmacol,  73  (8): (1215-24).  [PMID:17343831]
7. Łazewska D, Kuder K, Ligneau X, Camelin JC, Schunack W, Stark H, Kieć-Kononowicz K.  (2009)  Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands..  Bioorg Med Chem,  17  (8): (3037-42).  [PMID:19329325]
8. Schwartz JC.  (2011)  The histamine H3 receptor: from discovery to clinical trials with pitolisant..  Br J Pharmacol,  163  (4): (713-21).  [PMID:21615387]
9. Kollb-Sielecka M, Demolis P, Emmerich J, Markey G, Salmonson T, Haas M.  (2017)  The European Medicines Agency review of pitolisant for treatment of narcolepsy: summary of the scientific assessment by the Committee for Medicinal Products for Human Use..  Sleep Med,  33  (3): (125-129).  [PMID:28449891]
10. Szakacs Z, Dauvilliers Y, Mikhaylov V, Poverennova I, Krylov S, Jankovic S, Sonka K, Lehert P, Lecomte I, Lecomte JM et al..  (2017)  Safety and efficacy of pitolisant on cataplexy in patients with narcolepsy: a randomised, double-blind, placebo-controlled trial..  Lancet Neurol,  16  (3): (200-207).  [PMID:28129985]

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