Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H31Cl2N3O5.2ClH |
| Molecular Weight | 597.359 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CCOC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=CC(Cl)=C(OCCN3CCN(C)CC3)C(Cl)=C2O
InChI
InChIKey=JUJAUEQJEWIWCQ-FJSYBICCSA-N
InChI=1S/C25H31Cl2N3O5.2ClH/c1-3-34-25(33)20(15-17-7-5-4-6-8-17)28-24(32)18-16-19(26)23(21(27)22(18)31)35-14-13-30-11-9-29(2)10-12-30;;/h4-8,16,20,31H,3,9-15H2,1-2H3,(H,28,32);2*1H/t20-;;/m0../s1
JTE-607 is a multiple cytokine inhibitor. JTE-607 inhibited inflammatory cytokine production, including tumour necrosis factor (TNF)-alpha, interleukin IL-1beta, IL-6, IL-8, and IL-10, from LPS-stimulated human PBMCs. This compound may be useful for the treatment of various cytokine-mediated diseases such as septic shock without causing immunosuppression. JTE-607 may thus be efficacious in cytokine-mediated lung inflammation such as acute respiratory distress syndrome. JTE-607 inhibits the production of IL-10, IL-1ra and C-reactive protein in a human model of endotoxemia. In a leukaemia model engrafted with U-937 cells, JTE-607 significantly prolonged survival in mice and reduced human cytokine mRNA levels in the bone marrow. These results suggest the usefulness of JTE-607 in therapeutic applications for patients with hypercytokinemia and aggressive acute myelogenous leukaemia cell proliferation. JTE-607 had been in phase II clinical trials for the treatment of systemic inflammatory response syndrome but this study was discontinued.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| JTE-607, a novel inflammatory cytokine synthesis inhibitor without immunosuppression, protects from endotoxin shock in mice. | 1999 Aug |
|
| Prophylactic effect of JTE-607 on LPS-induced acute lung injury in rats with CINC-1 inhibition. | 2002 Mar |
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| Prior burn insult induces lethal acute lung injury in endotoxemic mice: effects of cytokine inhibition. | 2003 Feb |
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| Comparative study of glucocorticoids, cyclosporine A, and JTE-607 [(-)-Ethyl-N[3,5-dichloro-2-hydroxy-4-[2-(4-methylpiperazin-1-yl)ethoxy]benzoyl]-L-phenylalaninate dihydrochloride] in a mouse septic shock model. | 2004 Dec |
|
| Pharmacologic preconditioning of JTE-607, a novel cytokine inhibitor, attenuates ischemia-reperfusion injury in the myocardium. | 2004 Jun |
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| JTE-607, a cytokine release blocker, attenuates acid aspiration-induced lung injury in rats. | 2004 Mar 19 |
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| JTE-607, a multiple cytokine production inhibitor, ameliorates disease in a SCID mouse xenograft acute myeloid leukemia model. | 2006 Oct |
|
| JTE-607, an inflammatory cytokine synthesis inhibitor, attenuates ischemia/reperfusion-induced renal injury by reducing neutrophil activation in rats. | 2008 Jul |
|
| JTE-607, a multiple cytokine production inhibitor, induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells. | 2010 Mar |
|
| Effects of a cytokine inhibitor, JTE-607, on the response to endotoxin in healthy human volunteers. | 2011 Nov |
Patents
Sample Use Guides
0.03, 0.1 or 0.3 mg/kg/h a single 8-hour infusion
Route of Administration:
Intravenous
U-937 and HL-60 cells were exposed to 0.01–1 uM of JTE-607 for 2 h in the measurement of cytokine mRNA levels or 24 h to determine cytokine protein levels in the culture supernatant. IL-6 and IL-8 mRNA levels were reduced by JTE-607 from a concentration of 0.1 uM in both cell lines.
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2B68H6BWCX
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188791-09-5
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167629
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9938544
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ACTIVE MOIETY
SUBSTANCE RECORD
