CAS |
No.245747-71-1 |
英文名称 |
NFAT Transcription Factor Regulator-1 |
分子式 |
C17H10F6N4O2 |
分子量 |
416.28 |
溶解性 |
Soluble in DMSO |
纯度 |
≥98% |
外观(性状) |
Light yellow to yellow Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
运输条件 |
冷藏运输 |
SMILES |
O=C(C1=C(F)C=NC=C1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3OC(F)F)C=C2 |
InChIKey |
XGCRLPUGFWHAGJ-UHFFFAOYSA-N |
InChI |
InChI=1S/C17H10F6N4O2/c18-12-8-24-6-5-11(12)15(28)25-9-1-3-10(4-2-9)27-14(29-16(19)20)7-13(26-27)17(21,22)23/h1-8,16H,(H,25,28) |
PubChem CID |
9931706 |
靶点 |
IL-2 |
通路 |
Immunology & Inflammation |
背景说明 |
是 IL-2 合成 的抑制剂。 |
生物活性 |
NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC50 of 182 nM.[1] |
In Vitro |
NFAT Transcription Factor Regulator-1 (compound example 19) inhibits IL-2 synthesis with an IC50 of 182 nM. NFAT Transcription Factor Regulator-1 inhibits human and rat PBMC proliferation with IC50s of 82 and 146 nM, respectively. NFAT Transcription Factor Regulator-1 is able to inhibit IL-4 and IL-5 production in human T-cell lines with similar potency to its effects on IL-2 release[1]. |
In Vivo |
NFAT Transcription Factor Regulator-1 is found to have an inhibitory potency approximately 10-fold better than that of cyclosporine. Comparable inhibitory effects on T-cell IL-2 production are obtained with NFAT Transcription Factor Regulator-1 and cyclosporine at doses of 3.0 and 30 mg/kg, po, respectively. The efficacies achieved in monkeys in vivo for blocking T-cell cytokine production suggest that NFAT Transcription Factor Regulator-1 has potential similar to that of cyclosporine for use in transplantation[1]. |
动物实验 |
Monkey[1]Cynomolgus monkeys are bled to obtain heparinized baseline samples for measuring predrug cytokine production and then briefly intubated for intragastric dosing. Cyclosporine is administered in the Neoral formulation. Compound 19 is given. Postdrug blood samples are similarly obtained 2 h later. The samples are stimulated by spiking undiluted blood with PMA (50 ng/mL) and ionomycin (1μg/mL) and incubating for 24 h. Plasma samples are collected by centrifugation, and IL-2 concentrations are determined by ELISA using recombinant human IL-2 as standard[1]. |
数据来源文献 |
[1]. Djuric SW, et al. 3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator. J Med Chem. 2000 Aug 10;43(16):2975-81. |
规格 |
1mg 5mg 10mg 25mg 50mg |
单位 |
瓶 |