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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

Licofelone

Cayman Chemical Item Number 10007692

ML 3000 (CAS 156897-06-2)

Licofelone (CAS 156897-06-2)

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Description

Cross-talk between lipoxygenase (LO) and cyclooxygenase (COX) pathways has been observed in human osteoarthritic synovial explants which creates an arachidonic acid shunting phenomenon, stimulating interleukin-1β (IL-1β) synthesis. Licofelone is a dual inhibitor of COX and LO pathways, that decreases levels of prostaglandin E2, leukotriene B4, and lipoxins and prevents lipopolysaccharide-stimulated IL-1β expression.1 The IC50 values for inhibition of human thrombocyte COX and human 5-LO are 0.16 µM and 0.23 µM, respectively.2 Unlike other non-steroidal anti-inflammatory drugs, licofelone causes little or no damage to the gastric mucosa in rabbit parietal cells. This is presumably the result of licofelone’s affects on acid-secretory mechanisms, mediated by the inhibition of 5-LO activity.3

1 Marcouiller, P., Pelletier, J., Guévremont, M., et al. Leukotriene and prostaglandin synthesis pathways in osteoarthritic synovial membranes: Regulating factors for interleukin 1β synthesis. J Rheumatol 32(4) 704-712 (2005).

2 Laufer, S.A., Augustin, J., Dannhardt, G., et al. (6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase. J Med Chem 37 1894-1897 (1994).

3 Smolka, A.J., Goldenring, J.R., Gupta, S., et al. Inhibition of gastric H,K-ATPase activity and gastric epithelial cell IL-8 secretion by the pyrrolizine derivative ML 3000. BMC Gastroenterol 4(4) 1-11 (2004).

Synonyms
  • ML 3000
Formal Name 6-​(4-​chlorophenyl)-​2,​3-​dihydro-​2,​2-​dimethyl-​7-​phenyl-​1H-​pyrrolizine-​5-​acetic acid
CAS Number 156897-06-2
Molecular Formula C23H22ClNO2
Formula Weight 379.9
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere
SMILES
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CC1(C)​CC2=C(C3=CC=CC=C3)​C(C4=CC=C(Cl)​C=C4)​=C(CC(O)​=O)​N2C1

Background Reading

Marcouiller, P., Pelletier, J., Guévremont, M., et al. Leukotriene and prostaglandin synthesis pathways in osteoarthritic synovial membranes: Regulating factors for interleukin 1β synthesis. J Rheumatol 32(4) 704-712 (2005).

Smolka, A.J., Goldenring, J.R., Gupta, S., et al. Inhibition of gastric H,K-ATPase activity and gastric epithelial cell IL-8 secretion by the pyrrolizine derivative ML 3000. BMC Gastroenterol 4(4) 1-11 (2004).

Laufer, S.A., Augustin, J., Dannhardt, G., et al. (6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase. J Med Chem 37 1894-1897 (1994).
Size Price Quantity Subtotal
1 mg $43.00 $0.00
5 mg $194.00 $0.00
10 mg $344.00 $0.00
50 mg $1,505.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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