SAFit2 is a selective inhibitor of FKBP51 (FK506-binding protein 51), a cochaperone involved in stress hormone signaling, pain processing, and metabolic regulation. It binds FKBP51 with high affinity (Ki ≈ 6 nM) and displays >10-fold selectivity over the closely related FKBP52. In cell-based assays, SAFit2 effectively disrupts FKBP51–Hsp90 interactions, modulating glucocorticoid receptor activity and reducing downstream stress responses. In vivo, SAFit2 has shown analgesic effects in models of neuropathic and inflammatory pain, as well as antidepressant-like activity in stress-induced behavioral models, without impairing FKBP52-associated pathways. Its pharmacokinetic profile is suitable for systemic administration, with good brain penetration and minimal off-target effects.
MedKoo Cat#: 562643
Name: SAFit2
CAS#: 1643125-33-0
Chemical Formula: C46H62N2O10
Exact Mass: 802.4404
Molecular Weight: 803.00
Elemental Analysis: C, 68.80; H, 7.78; N, 3.49; O, 19.92
The following data is based on the product molecular weight 803.00 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
