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B7/CD28 interaction inhibitor 1

Names

[ CAS No. ]:
635324-72-0

[ Name ]:
B7/CD28 interaction inhibitor 1

[Synonym ]:
Dipyrazolo[3,4-b:3',4'-d]pyridin-3(2H)-one, 2-(4-fluorophenyl)-1,6-dihydro-6-methyl-4-[3-(trifluoromethyl)phenyl]-
2-(4-Fluorophenyl)-6-methyl-4-[3-(trifluoromethyl)phenyl]-1,6-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(2H)-one
CTLA-4 - INHIBITOR

Biological Activity

[Description]:

B7/CD28 interaction inhibitor 1 is a potent B7.1-CD28 interaction inhibitor with an IC50 of 50 nM[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology

[Target]

IC50: 50 nM (B7.1-CD28 interaction)[1]


[In Vitro]

Bivalent CTLA4 homodimers bridge bivalent B7.1 homodimers to form an unusually stable signaling complex. Blocking B7/CD28 interactions with monoclonal antibodies or soluble receptors results in immunosuppression and enhanced allograft survival, while B7/CTLA-4 blockade results in enhanced antitumor immune responses. The interaction of co-stimulatory molecules on T cells with B7 molecules on antigen presenting cells plays an important role in the activation of naive T cells. Consequently, agents that disrupt these interactions should have applications in treatment of transplant rejection as well as autoimmune diseases[1].

[References]

[1]. Green NJ, et al. Structure-activity studies of a series of dipyrazolo[3,4-b:3',4'-d]pyridin-3-ones binding to the immune regulatory protein B7.1. Bioorg Med Chem. 2003 Jul 3;11(13):2991-3013.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
599.5±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H13F4N5O

[ Molecular Weight ]:
427.354

[ Flash Point ]:
316.4±32.9 °C

[ Exact Mass ]:
427.105621

[ LogP ]:
3.80

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.677

[ Storage condition ]:
-20℃

Related Compounds