SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51) with a Ki value of 6 nM. SAfit2 has been used as a potential agent in the study of major depression, obesity, and chronic pain.
| Molecular Weight | 802.99 |
| Formula | C46H62N2O10 |
| CAS Number | 1643125-33-0 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | Powder -20°C |
| 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 FKBP (FK506-binding protein) Products |
|---|
| Suc-Ala-Leu-Pro-Phe-pNA
Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) is a substrate of FK-506 binding protein (FKBP). |
| RapaBlock
RapaBlock is a potent, non-immunosuppressive and brain-impermeable FKBP12 ligand. |
| FKBP51F67V-selective antagonist Ligand2
FKBP51F67V-selective antagonist Ligand2 is a potent FKBP51 F67V-selective antagonist ligand. |
| dTAGV-1-NEG TFA
dTAGV-1-NEG TFA is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1-NEG TFA is an FKBP12F36V-selective degrader. |
| AP1867
AP1867 is a synthetic FKBP12F36V-directed ligand. |
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