635324-72-0
中文名稱
CTLA-4 - INHIBITOR
英文名稱
2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one
CAS
635324-72-0
分子式
C21H13F4N5O
分子量
427.35
MOL 文件
635324-72-0.mol
更新日期
2024/11/12 15:28:25
635324-72-0 結(jié)構(gòu)式
基本信息
中文別名
2-(4-氟苯基)-6-甲基-4-(3-(三氟甲基)苯基)-1,2-二氫二吡唑并[3,4-B:3',4'-D]吡啶-3(6H)-酮 英文別名
MDK24720CTLA-4 - INHIBITO
CTLA-4 inhibitor 1
CTLA-4 - INHIBITOR
B7/CD28 interaction inhibitor 1
2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b
2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one
Dipyrazolo[3,4-b:3',4'-d]pyridin-3(2H)-one, 2-(4-fluorophenyl)-1,6-dihydro-6-methyl-4-[3-(trifluoromethyl)phenyl]-
物理化學(xué)性質(zhì)
沸點599.5±60.0 °C(Predicted)
密度1.54±0.1 g/cm3(Predicted)
儲存條件Sealed in dry,Room Temperature
酸度系數(shù)(pKa)5.76±0.20(Predicted)
形態(tài)Solid
顏色Off-white to light yellow
常見問題列表
生物活性
MDK 24720 (CTLA-4 inhibitor, copmound 6b) 是一種 Cytotoxic T-Lymphocyte-Associated protein 4 (CTLA-4, CD152) 的抑制劑，對B7.1–CD28的抑制作用的IC50值為50 nM。靶點
| Target | Value |
|
CD152
() | |
|
B7.1–CD28
(Cell-free assay) | 50 nM |
體外研究
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.