1246525-60-9 Usage
Uses
SR 1078 is a selective agonist of RORα and RORγ that stimulates ROR transcriptional activity in HEK293 cell reporter assays.
Biological Activity
sr1078 is an agonist of retinoic acid receptor-related orphan receptor (ror) rorα and rorγ with ic50 values of both 1-3 μm [1].rorα and rorγ are two members of nuclear receptor superfamily, which possesses a highly conserved dna-binding and a ligand-binding domain. these two receptors are considered to play important roles in the regulation of metabolism and the function of immune system [1].sr1078 is a selective rorα and rorγ agonist, which activate rorα and rorγ directed transcription via inducing conformational changes [1].sr1078 selectively targets on rorα and rorγ as an agonist but not on lxr and fxr [1]. it was shown that sr1078 was able to stimulate ror activity and subsequent ror-directed mrna expression. when hepg2 cells were treated with sr1078 for 24h, the ror directed reporter gene fg21 mrna level was increased by 3-fold, while another reporter gene g6pase was increased by 2-fold [1].in mouse model, i.p. injection of 10 mg/kg sr1078 for 1 hr resulted in 3.6 μm plasma concentration., and after 8 hr the concentration still sustained at 800 nm. i.p. injection of 10 mg/kg sr1078 for 2 hr resulted in significantly increased level of mrna of reporter gene g6pase and fg21 [1].
references
[1] wang y et al. , identification of a synthetic agonist for the orphan nuclear receptors rorα and rorγ, sr1078. acs chem biol., 2010, 5(11): 1029-1034.
Check Digit Verification of cas no
The CAS Registry Mumber 1246525-60-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,4,6,5,2 and 5 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1246525-60:
(9*1)+(8*2)+(7*4)+(6*6)+(5*5)+(4*2)+(3*5)+(2*6)+(1*0)=149
149 % 10 = 9
So 1246525-60-9 is a valid CAS Registry Number.
1246525-60-9Relevant articles and documents
Structure-based design of substituted hexafluoroisopropanol- arylsulfonamides as modulators of RORc
Fauber, Benjamin P.,De Leon Boenig, Gladys,Burton, Brenda,Eidenschenk, Celine,Everett, Christine,Gobbi, Alberto,Hymowitz, Sarah G.,Johnson, Adam R.,Liimatta, Marya,Lockey, Peter,Norman, Maxine,Ouyang, Wenjun,Rene, Olivier,Wong, Harvey
supporting information, p. 6604 - 6609 (2014/01/06)
The structure-activity relationships of T0901317 analogs were explored as RORc inverse agonists using the principles of property- and structure-based drug design. An X-ray co-crystal structure of T0901317 and RORc was obtained and provided molecular insight into why T0901317 functioned as an inverse agonist of RORc; whereas, the same ligand functioned as an agonist of FXR, LXR, and PXR. The structural data was also used to design inhibitors with improved RORc biochemical and cellular activities. The improved inhibitors possessed enhanced selectivity profiles (rationalized using the X-ray crystallographic data) against other nuclear receptors.