UPF 648
- Product Name
- UPF 648
- CAS No.
- 213400-34-1
- Chemical Name
- UPF 648
- Synonyms
- DBCC;UPF648;UPF 648;UPF648,UPF 648;(1S,2S)-2-(3,4-Dichlorobenzoyl)cyclopropanecarboxylic acid;Cyclopropanecarboxylic acid, 2-(3,4-dichlorobenzoyl)-, (1S,2S)-
- CBNumber
- CB42667175
- Molecular Formula
- C11H8Cl2O3
- Formula Weight
- 259.09
- MOL File
- 213400-34-1.mol
UPF 648 Property
- Boiling point:
- 461.3±45.0 °C(Predicted)
- Density
- 1.556±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: soluble
- form
- A solid
- pka
- 3.89±0.11(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 4926
- Product name
- UPF648
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $325
- Updated
- 2021/12/16
- Product number
- U800080
- Product name
- UPF648
- Packaging
- 10mg
- Price
- $285
- Updated
- 2021/12/16
- Product number
- Axon2118
- Product name
- UPF648
- Purity
- 99%
- Packaging
- 2mg
- Price
- $115.5
- Updated
- 2021/12/16
- Product number
- CD31002677
- Product name
- UPF-648
- Purity
- 98+%
- Packaging
- 5mg
- Price
- $243
- Updated
- 2021/12/16
- Product number
- CD31002677
- Product name
- UPF-648
- Purity
- 98+%
- Packaging
- 10mg
- Price
- $347
- Updated
- 2021/12/16
UPF 648 Chemical Properties,Usage,Production
Uses
UPF-648 is a kynurenine 3-monooxygenase (KMO) inhibitor. KMO is a key enzyme that is part of the kynurenine pathway, which is a metabolic pathway that utilizes tryptophan to produce nicotinamide adenine dinucleotide (NAD+). KMO is a potential therapeutic target for treating neurodegenerative and psychiatric disorders.
Biological Activity
UPF-648 is a potent, active site-targeting kynurenine 3-monooxygenase (KMO; kynurenine 3-hydroxylase) inhibitor (IC50 = 20 nM) th at prevents productive binding of the substrate L-kynurenine by perturbing the local active-site structure. UPF-648 protects against neurodegeneration in a murine (30 mg/kg, i.p.) and a Drosophila (100 μM in maize media) model of Huntingtonμs disease by shifting kynurenine pathway metabolism towards enhanced neuroprotective kynurenic acid (KYNA) formation and away from the free radicals generator 3-hydroxykynurenine (3-HK) and the excitotoxic quinolinic acid (QUIN).
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[1].
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[2].
UPF 648, has an IC50 of 20 nM and provides protection against intrastriatal QUIN injections in kynurenine aminotransferase (KAT II) deficient mice. UPF 648 treatment also shifts KP metabolism towards enhanced neuroprotective KYNA formation[3].
storage
Store at +4°C
UPF 648 Preparation Products And Raw materials
Raw materials
Preparation Products
UPF 648 Suppliers
- Tel
- --
- Fax
- --
- customerservice@tocris.co.uk
- Country
- United Kingdom
- ProdList
- 5726
- Advantage
- 77