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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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $293 | In Stock | |
| 5 mg | $722 | 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 | Rat H3LR:2.9 nM (Ki), Human H3LR: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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