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UCB-9260

Cat. No. M11009
UCB-9260 Structure
Synonym:

UCB9260

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Biological Activity

UCB-9260 is an orally active small molecule that inhibits tumor necrosis factor (TNF) signaling through an asymmetrical form of a stable trimer. UCB-9260 is more selective to tumor necrosis factor than other superfamily members and binds to tumor necrosis factor Kd The value is 13 nM.

Chemical Information
Molecular Weight 423.51
Formula C26H25N5O
CAS Number 1515888-53-5
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] James O'Connell, et al. Nat Commun . Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer

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