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) Y Key: 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).
Infobox references
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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.
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Receptor (ligands) | BLTTooltip Leukotriene B4 receptor | BLT1Tooltip Leukotriene B4 receptor 1 |
- Antagonists: 20-Carboxy-LTB4
- Amelubant
- CGS-23131 (LY-223982)
- CGS-25019C
- CP-105696
- CP-195543
- LY-293111
- Moxilubant
- ONO-4057
- RG-14893
- RP-69698
- SB-209247
- SC-53228
- Ticolubant
- U-75302
- ZK-158252
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BLT2Tooltip Leukotriene B4 receptor 2 |
- Antagonists: CP-195543
- LY-255283
- ZK-158252
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CysLTTooltip Cysteinyl leukotriene receptor | CysLT1Tooltip 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
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CysLT2Tooltip Cysteinyl leukotriene receptor 2 |
- Antagonists: BAYu9773
- BAYu9916
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CysLTETooltip Cysteinyl leukotriene receptor E | |
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Enzyme (inhibitors) | 5-LOXTooltip Arachidonate 5-lipoxygenase |
- FLAPTooltip Arachidonate 5-lipoxygenase-activating protein inhibitors: AM-103
- AM-679
- BAYx1005
- MK-591
- MK-886
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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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- See also
- Receptor/signaling modulators
- Prostanoid signaling modulators
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PPARαTooltip Peroxisome proliferator-activated receptor alpha | |
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PPARδTooltip Peroxisome proliferator-activated receptor delta |
- Antagonists: FH-535
- GSK-0660
- GSK-3787
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PPARγTooltip Peroxisome proliferator-activated receptor gamma |
- Antagonists: FH-535
- GW-9662
- SR-202
- T-0070907
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Non-selective | |
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- See also
- Receptor/signaling modulators
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