PF-02413873 is a potent, selective and fully competitive non-steroidal progesterone receptor (PR) antagonist that blocks progesterone binding and PR nuclear translocation. PF-02413873 suppresses endometrial growth in the macaque and human.
| Molecular Weight | 359.44 |
| Formula | C18H21N3O3S |
| CAS Number | 936345-35-6 |
| Solubility (25°C) | DMSO: 2 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.
[2] Hannah M Jones, et al. Application of PBPK modelling in drug discovery and development at Pfizer
| Related Progesterone Receptor Products |
|---|
| Trimegestone
Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. |
| Nomegestrol
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity. |
| Allylestrenol
Allylestrenol is an anabolic steroid with progesterone activity and potential physiologic function as a progesterone receptor agonist that can be used in studies related to preterm labor. |
| Cridanimod
Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression. Cridanimod is a small-molecule immunomodulator and interferon inducer. |
| Asoprisnil
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
