(2S,5S)-CMI-392
(2S,5S)-CMI-392 is the absolute configuration of CMI-392 (HY-19205A). CMI-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.
For research use only. We do not sell to patients.
- CAS No.: 205654-37-1
- Formula: C31H37ClN2O8S
- Molecular Weight:633.15
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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5-Lipoxygenase 100 nM (IC50) |
(2S,5S)-CMI-392 is the absolute configuration of CMI-392 (HY-19205A). CMI-392 potently inhibits the specific binding of [3H] PAF to cell membranes of CHO cells expressing human PAF receptors, with an IC50 of 10 nM; it inhibits 5-lipoxygenase activity in RBL-2H3 cell extracts, with an IC50 of 100 nM; it suppresses the production of LTB4 in human whole blood activated by calcium ionophore, with an IC50 of 7.8 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(2S,5S)-CMI-392 is the absolute configuration of CMI-392 (HY-19205A). CMI-392 (administered orally) dose-dependently alleviates the severity of dextran sulfate sodium (DSS)-induced colitis injury in mice and also inhibits ocular inflammatory responses in a rabbit eye model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 205654-37-1
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Molecular Weight 633.15
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Formula C31H37ClN2O8S
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SMILES
CN(O)C(NCC1=C(OCCSC2=CC=C(C=C2)Cl)C(OC)=CC([C@H]3O[C@H](C4=CC(OC)=C(C(OC)=C4)OC)CC3)=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(2S,5S)-CMI-392 Related Classifications
HY-19205B Related Classifications
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