From Wikipedia, the free encyclopedia
Etalocib
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Names
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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
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Other names
LY293111 VML 295
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Identifiers
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ChEMBL
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ChemSpider
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KEGG
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UNII
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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) YKey: YFIZRWPXUYFCSN-UHFFFAOYSA-N Y
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Fc1ccc(cc1)c4c(O)cc(OCCCOc3cccc(Oc2ccccc2C(=O)O)c3CCC)c(c4)CC
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Properties
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C33H33FO6
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Molar mass
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544.619 g·mol−1
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Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
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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
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^ 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.
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^ 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.
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^
"Etalocib". Adisinsight. Retrieved 31 January 2017.
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Receptor (
ligands) |
BLTTooltip Leukotriene B4 receptor |
BLT1Tooltip Leukotriene B4 receptor 1 | |
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BLT2Tooltip Leukotriene B4 receptor 2 | |
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CysLTTooltip Cysteinyl leukotriene receptor |
CysLT1Tooltip Cysteinyl leukotriene receptor 1 | |
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CysLT2Tooltip Cysteinyl leukotriene receptor 2 | |
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CysLTETooltip Cysteinyl leukotriene receptor E | |
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Enzyme (
inhibitors) |
5-LOXTooltip Arachidonate 5-lipoxygenase | |
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12-LOXTooltip Arachidonate 12-lipoxygenase | |
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15-LOXTooltip Arachidonate 15-lipoxygenase | |
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LTA4HTooltip Leukotriene A4 hydrolase | |
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LTB4HTooltip Leukotriene B4 ω-hydroxylase | |
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LTC4STooltip Leukotriene C4 synthase | |
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LTC4HTooltip Leukotriene C4 hydrolase | |
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LTD4Tooltip Leukotriene D4 hydrolase | |
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Others | |
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PPARαTooltip Peroxisome proliferator-activated receptor alpha | |
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PPARδTooltip Peroxisome proliferator-activated receptor delta | |
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PPARγTooltip Peroxisome proliferator-activated receptor gamma | |
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Non-selective | |
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