UPF-648 (sodiuM salt)
- CAS No.
- 1465017-87-1
- Chemical Name:
- UPF-648 (sodiuM salt)
- Synonyms
- UPF-648 (sodiuM salt);UPF 648 sodium salt,UPF648 sodium salt
- CBNumber:
- CB62735544
- Molecular Formula:
- C11H9Cl2NaO3
- Molecular Weight:
- 283.08
- MDL Number:
- MFCD28385854
- MOL File:
- 1465017-87-1.mol
- MSDS File:
- SDS
- TDS File:
- TDS
UPF-648 (sodiuM salt) Chemical Properties, Uses, Production
Uses
UPF-648 sodium salt is an effective inhibitor of kynurenine 3-monooxygenase (KMO), achieving approximately 81% inhibition at a concentration of 1uM, with no inhibitory effect on kynurenine aminotransferase (KAT).
Biological Activity
UPF-648 sodium salt is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.
in vitro
BFF 122 inhibited KAT activity almost completely at both 1 and 0.1 mM. The effect was still remarkable at 0.01 mM (70 ± 1 % inhibition). At the same three concentrations, BFF 122 did not affect KMO activity significantly. In contrast, UPF 648 totally blocked KMO at 0.1 and 0.01 mM and was still highly active at 0.001 mM (81 ± 10 % inhibition), but the compound was essentially ineffective at blocking KAT activity . UPF 648 binds close to the FAD cofactor and perturbs the local active-site structure, preventing productive binding of the substrate l-kynurenine. Functional assays and targeted mutagenesis reveal that the active-site architecture and UPF 648 binding are essentially identical in human KMO, validating the yeast KMO-UPF 648 structure as a template for structure-based drug design.
in vivo
Applying an identical experimental design, separate rats were used to study the effect of KMO inhibition on the de novo synthesis of KP metabolites in the lesioned striatum. These animals were bilaterally injected with 0.1 mM UPF 648 and 3H-kynurenine in PBS. 0.1 mM UPF 648 significantly reduced the neosynthesis of 3-HK and QUIN in the lesioned striatum (by 77 % and 66%, respectively) and moderately (27%) but significantly increased the de novo formation of KYNA. Administered to pregnant rats or mice on the last day of gestation, UPF 648 (50 mg/kg, i.p.) produced qualitatively similar changes (i.e., large increases in kynurenine and KYNA and reductions in 3-HK and QUIN) in the brain and liver of the offspring. Rat pups delivered by UPF 648-treated mothers and immediately exposed to neonatal asphyxia showed further enhanced brain KYNA levels .
target
KMO inhibitorin
References
[1] Amori L, et al. On the relationship between the two branches of the kynurenine pathway in the rat brain in vivo. J Neurochem. 2009 Apr;109(2):316-25. DOI:10.1111/j.1471-4159.2009.05893.x
[2] Ceresoli-Borroni G, et al. Perinatal kynurenine 3-hydroxylase inhibition in rodents: pathophysiological implications. J Neurosci Res. 2007 Mar;85(4):845-54. DOI:10.1002/jnr.21183
[3] Amaral M, et al. Structural basis of kynurenine 3-monooxygenase inhibition. Nature. 2013 Apr 18;496(7445):382-5. DOI:10.1038/nature12039
UPF-648 (sodiuM salt) Preparation Products And Raw materials
Raw materials
Preparation Products
UPF-648 (sodiuM salt) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4853 | 58 |
| LETOPHARM LIMITED | +86-21-5821 5861 | sales@letopharm.com | China | 2374 | 58 |
| Musechem | +1-800-259-7612 | info@musechem.com | United States | 4648 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| TargetMol Chemicals Inc. | 13564774135 | marketing@targetmol.com | United States | 19950 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 38999 | 58 |
| Supplier | Advantage |
|---|---|
| MedChemexpress LLC | 58 |
| LETOPHARM LIMITED | 58 |
| Musechem | 60 |
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
View Latest Price from UPF-648 (sodiuM salt) manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2026-04-20 | UPF-648 sodium salt
1465017-87-1
|
$1520.00-2500.00 | 10g | TargetMol Chemicals Inc. | |||
 |
2025-07-17 | UPF-648 sodium salt
1465017-87-1
|
$1520.00-2500.00 | 10g | TargetMol Chemicals Inc. |
-
- UPF-648 sodium salt
1465017-87-1
- $1520.00-2500.00
- TargetMol Chemicals Inc.
-
- UPF-648 sodium salt
1465017-87-1
- $1520.00-2500.00
- TargetMol Chemicals Inc.
