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Proxyfan (Proxifan) is a high-affinity protean antagonist/agonist of histamine H3 receptors with a full spectrum of pharmacological activity ranging from full agonist to full inverse agonist(antagonist), depending on the competition between constitutively active and resting H3 receptors within a given tissue or brain region.Proxyfan acts as a neutral antagonist in the feeding-associated ventral medial nucleus of the hypothalamus, and as a agonist in the basolateral amygdala of the rat (BLA).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $293 | In Stock | In Stock | |
| 5 mg | $722 | In Stock | In Stock | |
| 10 mg | $987 | - | In Stock | |
| 25 mg | $1,520 | - | In Stock | |
| 50 mg | $1,980 | - | In Stock | |
| 100 mg | $2,500 | - | In Stock |
| Description | Proxyfan (Proxifan) is a high-affinity protean antagonist/agonist of histamine H3 receptors with a full spectrum of pharmacological activity ranging from full agonist to full inverse agonist(antagonist), depending on the competition between constitutively active and resting H3 receptors within a given tissue or brain region.Proxyfan acts as a neutral antagonist in the feeding-associated ventral medial nucleus of the hypothalamus, and as a agonist in the basolateral amygdala of the rat (BLA). |
| Targets&IC50 | H3LR (rat):2.9 nM (Ki), H3LR (human):2.7 nM (Ki) |
| In vitro | Proxyfan is the neutral antagonist of histamine H3 receptors, with Ki values of 2.9 nM for rat and 2.7 nM for human H3 receptors. [1] |
| In vivo | The H3 receptor neutral antagonist Proxyfan was used in rats using intraperitoneal injection. Proxyfan (0.2–5.0 mg/kg) did not affect food intake in freely feeding rats during either the light or dark phase. At night, proxyfan antagonized the orexigenic effect of the H3 agonist imetit (10 mg/kg) and the anorectic effect of the inverse agonist thioperamide (2 mg/kg).[2] |
| Synonyms | Proxifan |
| Molecular Weight | 216.28 |
| Formula | C13H16N2O |
| Cas No. | 177708-09-7 |
| Smiles | N1=CNC(=C1)CCCOCC=2C=CC=CC2 |
| Relative Density. | 1.115g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4 mg/mL (18.49 mM), Sonication is recommended. H2O: 4 mg/mL (18.49 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO/H2O
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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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