PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.
| Molecular Weight | 440.49 |
| Formula | C22H21FN4O3S |
| CAS Number | 1614245-70-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL (ultrasonic) |
| Storage | 4°C, protect from light |
| 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 GABA Receptor Products |
|---|
| Alogabat
Alogabat (RG-7816) is a GABAA α5 receptor positive allosteric modulators (PAMs). |
| CGP7930
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. |
| 5-Aminovaleric acid
5-Aminovaleric acid is a GABA receptor antagonist. |
| L-2,4-Diaminobutyric acid dihydrochloride
L-2,4-Diaminobutyric acid dihydrochloride inhibits GABA transaminase activity, resulting in elevated GABA levels, and exhibits ex vivo antitumor activity against mouse fibrosarcoma cells. In addition, L-2,4-Diaminobutyric acid dihydrochloride can be used as an internal standard for amino acid analysis. |
| 3,4,5-Trimethoxy-trans-cinnamic acid
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
