117690-79-6 Usage
Description
Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B4 (LTB4) have been potential drug development targets for several years. The tetrazole LY255283 is a competitive antagonist of the BLT2 receptor. It displaces radiolabeled LTB4 from guinea pig lung membrane, with an IC50 of about 100 nM. LY255283 exhibits IC50 values of ~950 nM and >10 μM at human recombinant BLT2 and BLT1 receptors, respectively. LY255283 inhibits eosinophil chemotaxis by 80% at a concentration of 10 μM, and inhibits the binding of radiolabeled LTB4 to eosinophil membranes with an IC50 of 260 nM.
Uses
LY-255283 is a selective, competitive BLT2 receptor antagonist used in the treatment of chronic myeloid leukemia.
Biological Activity
Selective, competitive antagonist of BLT 2 receptors (IC 50 values are ~ 1 and > 10 μ M at human recombinant BLT 2 and BLT 1 receptors respectively). Inhibits LTB 4 -induced contraction of lung parenchyma (pA 2 = 7.2), and reduces LTB 4 -mediated airway obstruction in guinea pigs following i.v. and oral administration.
Check Digit Verification of cas no
The CAS Registry Mumber 117690-79-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,7,6,9 and 0 respectively; the second part has 2 digits, 7 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 117690-79:
(8*1)+(7*1)+(6*7)+(5*6)+(4*9)+(3*0)+(2*7)+(1*9)=146
146 % 10 = 6
So 117690-79-6 is a valid CAS Registry Number.
InChI:InChI=1/C19H28N4O3/c1-5-14-11-15(13(2)24)16(25)12-17(14)26-10-8-6-7-9-19(3,4)18-20-22-23-21-18/h11-12,25H,5-10H2,1-4H3,(H,20,21,22,23)
117690-79-6Relevant articles and documents
Discovery and SAR study of hydroxyacetophenone derivatives as potent, non-steroidal farnesoid X receptor (FXR) antagonists
Liu, Peng,Xu, Xing,Chen, Lili,Ma, Lei,Shen, Xu,Hu, Lihong
, p. 1596 - 1607 (2014/03/21)
Compound 1 (IC50 = 35.2 ± 7.2 μM), a moderate FXR antagonist was discovered via high-throughput screening. Structure-activity relationship studies indicated that the shape and the lipophilicity of the substituents of the aromatic ring affect the activity dramatically, increasing the shape and the lipophilicity of the substituents of the aromatic ring enhances the potency of FXR antagonists. Especially, when the OH at C2 position of the aromatic ring was replaced by the OBn substituent (analog 2b), its activity could be improved to IC50 = 1.1 ± 0.1 μM. Besides, the length of the linker and the tetrazole structure are essential for retaining the activity.
ANTI-INFLAMMATORY AGENTS
-
, (2008/06/13)
This invention provides benzene derivatives, pharmaceutical formulations of those derivatives, and a method of using the derivatives for the treatment of inflammation in mammals.
