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635324-72-0

635324-72-0 structure
635324-72-0 structure
  • Name: B7/CD28 interaction inhibitor 1
  • Chemical Name: 2-(4-Fluorophenyl)-6-methyl-4-[3-(trifluoromethyl)phenyl]-1,6-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(2H)-one
  • CAS Number: 635324-72-0
  • Molecular Formula: C21H13F4N5O
  • Molecular Weight: 427.354
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2018-06-26 20:12:13
  • Modify Date: 2024-04-03 12:23:33
  • B7/CD28 interaction inhibitor 1 is a potent B7.1-CD28 interaction inhibitor with an IC50 of 50 nM[1].

Name 2-(4-Fluorophenyl)-6-methyl-4-[3-(trifluoromethyl)phenyl]-1,6-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(2H)-one
Synonyms 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
Description B7/CD28 interaction inhibitor 1 is a potent B7.1-CD28 interaction inhibitor with an IC50 of 50 nM[1].
Related Catalog
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.

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℃