SP-13786 (UAMC-1110) is a novel potent and selective inhibitor of fibroblast activation protein (fap), displaying low nanomolar inhibitory potency and high selectivity against the related dipeptidyl peptidases (dpps) dppiv, dpp9, dppii, and prolyl oligopeptidase (prep). Pharmacokinetic evaluation in mice of SP-13786 demonstrates high oral bioavailability, plasma half-life, and the potential to selectively and completely inhibit FAP in vivo.
| Molecular Weight | 344.32 |
| Formula | C17H14F2N4O2 |
| CAS Number | 1448440-52-5 |
| Solubility (25°C) | DMSO ≥ 60 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.
| Related FAP Products |
|---|
| 3BP-3940
3BP-3940 is a highly potent fibroblast activation protein (FAP)-targeting peptide for theranostics. |
| NH2-UAMC1110 TFA
NH2-UAMC1110 TFA is a UAMC1110 derivative that can be used in the synthesis of FAPI-QS. |
| FAP-IN-1
FAP-IN-1 is a fibroblast activation protein (FAP) inhibitor with an IC50 value of 3.3 nM. |
| FAPI-74
FAPI-74 is a PET (positron emission tomography) tracer targeting the fibroblast activation protein (FAP). |
| FAP-IN-2 TFA
FAP-IN-2 TFA is a 99mTc-labeled isonitrile-containing FAP inhibitor derivative that can be used for tumor imaging. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
