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PF-03654764 exhibits high affinity for the human H3 receptor, but displays significantly lower affinity for the rat H3 receptor, with over 1000-fold selectivity against other human histamine receptor subtypes (H1, H2, and H4). In functional assays measuring cAMP using reporter gene assays (β-lactamase) conducted in HEK293 cells stably expressing the full-length human or rat H3 receptor, PF-03654764 demonstrated potent antagonist properties.

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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | PF-03654764 exhibits high affinity for the human H3 receptor, but displays significantly lower affinity for the rat H3 receptor, with over 1000-fold selectivity against other human histamine receptor subtypes (H1, H2, and H4). In functional assays measuring cAMP using reporter gene assays (β-lactamase) conducted in HEK293 cells stably expressing the full-length human or rat H3 receptor, PF-03654764 demonstrated potent antagonist properties. |
| Synonyms | Q27285769, OP970177FN |
| Molecular Weight | 350.46(free base) |
| Formula | C20H28F2N2O xC7H8O3S |
| Cas No. | 1337536-85-2 |
| Smiles | S(=O)(=O)(O)C1=CC=C(C)C=C1.F[C@@]1(C[C@@H](C(NCC(C)C)=O)C1)C2=CC(F)=C(CN3CCCC3)C=C2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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