PF-03654764
Based on 1 Customer Validation
PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research.
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- Pureté: 99.0%
- CAS No.: 935840-35-0
- Formule: C20H28F2N2O
- Masse moléculaire:350.45
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Voir tous les produits spécifiques à Isoform Histamine Receptor
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Activité biologique
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human H3 receptor 1.2 nM (Ki) |
rat H3 receptor 7.9 nM (Ki) |
human H3 receptor 8.98 (pKi) |
rat H3 receptor 8.10 (pKi) |
PF-03654764 has pKi values of 8.98 and 8.10 for human H3 and rat H3 in whole cell assay, respectively. PF-03654764 has pKi values of 8.84, 7.73 and Ki values of 1.4 nM and 19 nM for human H3 and rat H3 in HEK-293 cells, respectively. PF-03654764 has >1000-fold selectivity for the H3 receptor over the other histamine receptor subtypes[1].
PF-03654764 has a human liver microsomes (HLM) T1/2 of 120 min and a HLM CLh <5 mL/min kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PF-03654764 (1 mL/kg; oral; 7 days) has a Cmax of 6302 ng/mL and an AUC0-24 of 18175 ng h/mL in beagle dogs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 935840-35-0
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Appearance Solid
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Masse moléculaire 350.45
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Formule C20H28F2N2O
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Color White to off-white
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SMILES
O=C([C@@H]1C[C@@](C2=CC(F)=C(CN3CCCC3)C=C2)(F)C1)NCC(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Travis T Wager, et al. Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem. 2011 Nov 10;54(21):7602-20. [Content Brief]
[2]. Michelle L North, et al. Add-on histamine receptor-3 antagonist for allergic rhinitis: a double blind randomized crossover trial using the environmental exposure unit. Allergy Asthma Clin Immunol. 2014 Jul 3;10(1):33. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-03654764 Related Classifications
HY-123812 Related Classifications
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