193739-23-0
Chemical Structure
CMI-392
Synonym(s): LDP-392
- CAS No.: 193739-23-0
- Formula:C31H37ClN2O8S
- Molecular Weight:633.15
IUPAC Name: 3-(2-(2-((4-chlorophenyl)thio)ethoxy)-3-methoxy-5-((2S,5S)-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran-2-yl)benzyl)-1-hydroxy-1-methylurea
InChIKey: LZVBMKDVEPGGFK-DQEYMECFSA-N
SMILES: O=C(NCC1=CC([C@H]2O[C@H](C3=CC(OC)=C(OC)C(OC)=C3)CC2)=CC(OC)=C1OCCSC4=CC=C(Cl)C=C4)N(O)C
Biological Activity: CMI-392 (LDP-392) is an orally active dual 5-lipoxygenase inhibitor and platelet-activating factor receptor (PAFR) antagonist, with an IC50 of 10 nM for human PAF receptor and an IC50 of 100 nM for rat 5-lipoxygenase. CMI-392 blocks PAF receptor binding, inhibits leukotriene synthesis, attenuates PAF-induced hemoconcentration, and suppresses arachidonic acid- and TPA-induced ear swelling in mice. CMI-392 reduces inflammatory cell infiltration, decreases MPO levels, alleviates ocular inflammation, and improves dextran sulfate sodium-induced colitis. CMI-392 can be used in the research of inflammatory and immune-related diseases such as colitis and atopic dermatitis[1][2].
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CMI-392 | CMI-392 (LDP-392) is an orally active dual 5-lipoxygenase inhibitor and platelet-activating factor receptor (PAFR) antagonist, with an IC50 of 10 nM for human PAF receptor and an IC50 of 100 nM for rat 5-lipoxygenase. CMI-392 blocks PAF receptor binding, inhibits leukotriene synthesis, attenuates PAF-induced hemoconcentration, and suppresses arachidonic acid- and TPA-induced ear swelling in mice. CMI-392 reduces inflammatory cell infiltration, decreases MPO levels, alleviates ocular inflammation, and improves dextran sulfate sodium-induced colitis. CMI-392 can be used in the research of inflammatory and immune-related diseases such as colitis and atopic dermatitis. | |||||||||||||||||||||
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- [1]. Cai X, et al. (+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist. Journal of medicinal chemistry. 1998 May 21;41(11):1970-9. [Content Brief]
- [2]. Julémont F, et al. Recent developments in 5lipoxygenase inhibitors. Expert Opinion on Therapeutic Patents, 2003, 13(1):1-13.
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