PF-02413873

SKU: orb1304956

Description

PF-02413873 is a potent, competitive nonsteroidal progesterone receptor antagonist with a Ki of 2.6 nM. It is a valuable research tool for investigating progesterone receptor function in vitro and for exploring potential therapeutic applications in conditions like endometriosis in preclinical models.

Key Properties

• CAS Number: 936345-35-6
• MW: 359.44
• Purity: 99.90%
• Formula: C₁₈H₂₁N₃O₃S
• SMILES: Cc1c(Oc2cc(C)c(C#N)c(C)c2)c(nn1CS(C)(=O)=O)C1CC1
• Target: Progesterone Receptor
• Solubility: DMSO:95 mg/mL (264.3 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.56 mM)

Bioactivity

• Target IC50:
  Progesterone receptor:2.6 nM (Ki)
• In Vivo:
  In cynomolgus macaques, PF-02413873 (3 mg/kg; p.o.) exhibits a t1/2 of 4.2 h, a Cmax of 162 ng/mL and CL/F of 41 mL/min/kg. PF-02413873 (2.5 and 10 mg/kg; p.o.) reduces the endometrial thickness of 43 and 56%, respectively.
• In Vitro:
  PF-02413873 induces nuclear translocation only at high concentrations (>3 μM). PF-02413873 shows a derived Ki of 9.7 nM in the T47D native functional assay.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, NR3C3, nonsteroidal, nuclear, endometrial, Inhibitor, translocation, PF 02413873, PF2413873, PF-2413873, PF02413873, PF-02413873, PF 2413873, progesterone, ProgesteroneReceptor, Progesterone Receptor, progesterone receptor

Compound Identifiers

PubChem CID

16662425