PF 04457845 is a potent and selective irreversible FAAH inhibitor (IC50 = 7.2 nM). Selective for FAAH over a panel of other serine hydrolases. Exhibits efficacy in a rat inflammatory pain model. Orally bioavailable and brain penetrant.
| Molecular Weight | 455.43 |
| Formula | C23H20F3N5O2 |
| CAS Number | 1020315-31-4 |
| Solubility (25°C) | DMSO 45.54 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related FAAH Products |
|---|
| N-Benzyllinolenamide
N-Benzyllinolenamide is a natural macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 41.8 μM. |
| N-(3-Methoxybenzyl)palmitamide
N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders. |
| VU534
VU534 is a NAPE-PLD agonist with an EC50 of 0.30 μM.In addition, VU534 can dependently enhance Efferocytosis in macrophages. VU534 can be used in studies of cardiometabolic diseases. |
| MK-4409
MK-4409 is a potent oxazole FAAH inhibitor and can be used for the research of inflammatory and neuropathic pain. |
| N-Benzylpalmitamide
N-Benzylpalmitamide is a macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH). |
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