Names
Preferred IUPAC name
25 -Ethyl-14 -fluoro-22 -hydroxy-82 -propyl-3,7,9-trioxa-1,10(1),2(1,4),8(1,3)-tetrabenzenadecaphane-102 -carboxylic acid
Other names
LY293111 VML 295
Identifiers
ChEMBL
ChemSpider
KEGG
UNII
InChI=1S/C33H33FO6/c1-3-9-25-29(12-7-13-30(25)40-31-11-6-5-10-26(31)33(36)37)38-18-8-19-39-32-21-28(35)27(20-22(32)4-2)23-14-16-24(34)17-15-23/h5-7,10-17,20-21,35H,3-4,8-9,18-19H2,1-2H3,(H,36,37)
Y Key: YFIZRWPXUYFCSN-UHFFFAOYSA-N
Y
Fc1ccc(cc1)c4c(O)cc(OCCCOc3cccc(Oc2ccccc2C(=O)O)c3CCC)c(c4)CC
Properties
C 33 H 33 F O 6
Molar mass
544.619 g·mol−1
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
Etalocib is a drug candidate that was under development for the treatment of various types of cancer.[1] It acts as a leukotriene B4 receptor antagonist and a PPARγ agonist .[2]
Clinical trials were conducted measuring efficacy for treatment of non-small cell lung cancer and pancreatic cancer and the inflammatory conditions asthma , psoriasis , and ulcerative colitis , but were suspended due to lack of efficacy.[3]
References
^ Jänne, P. A.; Paz-Ares, L; Oh, Y; Eschbach, C; Hirsh, V; Enas, N; Brail, L; von Pawel, J (2014). "Randomized, double-blind, phase II trial comparing gemcitabine-cisplatin plus the LTB4 antagonist LY293111 versus gemcitabine-cisplatin plus placebo in first-line non-small-cell lung cancer" . Journal of Thoracic Oncology . 9 (1): 126–31. doi :10.1097/JTO.0000000000000037 . PMID 24346102 .
^ Adrian, T. E.; Hennig, R; Friess, H; Ding, X (2008). "The Role of PPARgamma Receptors and Leukotriene B(4) Receptors in Mediating the Effects of LY293111 in Pancreatic Cancer" . PPAR Research . 2008 : 827096. doi :10.1155/2008/827096 . PMC 2631651 . PMID 19190780 .
^ "Etalocib" . Adisinsight . Retrieved 31 January 2017 .
Receptor (ligands )
BLT Tooltip Leukotriene B4 receptor
BLT1 Tooltip Leukotriene B4 receptor 1
Antagonists: 20-Carboxy-LTB<sub>4</sub>
Amelubant
CGS-23131 (LY-223982)
CGS-25019C
CP-105696
CP-195543
Etalocib
LY-293111
Moxilubant
ONO-4057
RG-14893
RP-69698
SB-209247
SC-53228
Ticolubant
U-75302
ZK-158252
BLT2 Tooltip Leukotriene B4 receptor 2
Antagonists: CP-195543
LY-255283
ZK-158252
CysLT Tooltip Cysteinyl leukotriene receptor
CysLT1 Tooltip Cysteinyl leukotriene receptor 1
Antagonists: Ablukast
BAYu9773
BAYu9916
BAYx7195
Cinalukast
FPL-55712
ICI-198615
Iralukast
LY-170680
Masilukast
MK-571
Montelukast
ONO-1078
Pobilukast
Pranlukast
Ritolukast
SKF-104353
SR-2640
Sulukast
Tipelukast
Tomelukast
Verlukast
Zafirlukast
ZD-3523
CysLT2 Tooltip Cysteinyl leukotriene receptor 2
Antagonists: BAYu9773
BAYu9916
CysLTE Tooltip Cysteinyl leukotriene receptor E
Enzyme (inhibitors )
5-LOX Tooltip Arachidonate 5-lipoxygenase
FLAP Tooltip Arachidonate 5-lipoxygenase-activating protein inhibitors: AM-103
AM-679
BAYx1005
MK-591
MK-886
12-LOX Tooltip Arachidonate 12-lipoxygenase 15-LOX Tooltip Arachidonate 15-lipoxygenase LTA4 H Tooltip Leukotriene A4 hydrolase LTB4 H Tooltip Leukotriene B4 ω-hydroxylase LTC4 S Tooltip Leukotriene C4 synthase LTC4 H Tooltip Leukotriene C4 hydrolase LTD4 Tooltip Leukotriene D4 hydrolase
Others
PPARα Tooltip Peroxisome proliferator-activated receptor alpha PPARδ Tooltip Peroxisome proliferator-activated receptor delta
Antagonists: FH-535
GSK-0660
GSK-3787
PPARγ Tooltip Peroxisome proliferator-activated receptor gamma
Antagonists: FH-535
GW-9662
SR-202
T-0070907
Non-selective
This page was last edited on 3 October 2022, at 03:03