Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
Other Sizes |
|
UCB-9260 (UCB9260; UCB 9260) is an oral anti-inflammatory drug that may be used to treat autoimmune conditions like Crohn's disease and rheumatoid arthritis. It functions as a TNF inhibitor, preventing TNF signaling by maintaining an asymmetric form of the trimer. After stimulating Hek-293 cells with TNF (10 pM), UCB-9260 inhibits NF-κB in vitro with a geometric mean IC50 of 202 nM. In a mouse rheumatoid arthritis-CIA model, UCB-9260 significantly lowers the clinical score in vivo.
Targets |
TNF (Kd = 13 nM); NF-κB (Kd = 202 nM)
|
|
---|---|---|
ln Vitro |
|
|
ln Vivo |
|
|
References |
Molecular Formula |
C26H25N5O
|
---|---|
Molecular Weight |
423.509605169296
|
Exact Mass |
423.21
|
Elemental Analysis |
C, 73.74; H, 5.95; N, 16.54; O, 3.78
|
CAS # |
1515888-53-5
|
Related CAS # |
1515888-53-5
|
PubChem CID |
72700327
|
Appearance |
Brown to gray solid
|
LogP |
3.5
|
Hydrogen Bond Donor Count |
1
|
Hydrogen Bond Acceptor Count |
4
|
Rotatable Bond Count |
5
|
Heavy Atom Count |
32
|
Complexity |
613
|
Defined Atom Stereocenter Count |
0
|
InChi Key |
RZGFWGNCSYUEPR-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C26H25N5O/c1-17-4-5-18(2)21(12-17)16-31-24-13-20(22-14-28-30(3)15-22)6-7-23(24)29-26(31)25(32)19-8-10-27-11-9-19/h4-15,25,32H,16H2,1-3H3
|
Chemical Name |
[1-[(2,5-dimethylphenyl)methyl]-6-(1-methylpyrazol-4-yl)benzimidazol-2-yl]-pyridin-4-ylmethanol
|
Synonyms |
UCB-9260; UCB9260; UCB 9260
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: 85~125 mg/mL (200.7~295.2 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (14.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3612 mL | 11.8061 mL | 23.6122 mL | |
5 mM | 0.4722 mL | 2.3612 mL | 4.7224 mL | |
10 mM | 0.2361 mL | 1.1806 mL | 2.3612 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.