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Chemical Structure| 118414-82-7 Chemical Structure| 118414-82-7
Chemical Structure| 118414-82-7

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CAS No.: 118414-82-7

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MK886 is an inhibitor of 5-lipoxygenase activating protein (FLAP), PPARα, and the biosynthesis of leukotriene (LT).

Synonyms: L 663536; L-663,536

4.5 *For Research Use Only !

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Product Details of MK-886

CAS No. :118414-82-7
Formula : C27H34ClNO2S
M.W : 472.08
SMILES Code : O=C(O)C(C)(C)CC(N1CC2=CC=C(Cl)C=C2)=C(SC(C)(C)C)C3=C1C=CC(C(C)C)=C3
Synonyms :
L 663536; L-663,536
MDL No. :MFCD00876710
InChI Key :QAOAOVKBIIKRNL-UHFFFAOYSA-N
Pubchem ID :3651377

Safety of MK-886

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • lipoxygenase

In Vitro:

Cell Line
Concentration Treated Time Description Reference
J774.1 macrophages 50 μg/mL 24 hours PGE2 pre-treatment enhanced TsV-induced IL-1β expression, while EP2 and EP4 antagonists abrogated IL-1β production. PMC4766425
Bone marrow-derived macrophages (BMDMs) 50 μg/mL 24 hours TsV alone induces significant production of IL-1β, demonstrating that the venom itself delivers signals necessary for inflammasome activation in BMDMs. PMC4766425
C91/PL cells 200 nM 30 minutes To evaluate the effect of LTB4 secretion on Jurkat cell migration. Results showed that the supernatant of C91/PL cells significantly attracted Jurkat cell migration, while the supernatant of drug-treated C91/PL cells had reduced chemotactic capacity. PMC5489682
Jurkat cells 200 nM 30 minutes Investigate Nr1d1 binding to the GATA3 promoter region in human Jurkat cells PMC5489682
Rat pulmonary vascular endothelial cells 10^-5 M 10 minutes MK-886 significantly reduced the pressor responses induced by angiotensin II and hypoxia PMC507334

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice (C57BL/6) TsV-induced inflammation model Intraperitoneal 5 mg/kg 4 h and 0.5 h before and again 4 and 8 h after To assess the effect of MK886 on TsV-induced inflammation and mortality. Results showed that MK886 increased mortality, decreased LTB4 and IL-1β, and increased PGE2 levels. PMC4766425
Mice Acetic acid-induced visceral pain model Subcutaneous injection 1 mg/kg Single administration MK-886, as a PPAR-α antagonist, blocked the analgesic effects of URB937 in the acetic acid-induced visceral pain model PMC3260554
Humanized mice HTLV-1 infection model Intraperitoneal injection 5 nmol/mouse Three times a week for 6 weeks Reduce HTLV-1 proviral load and number of infected clones PMC5489682
Rats Chronic hypoxic pulmonary hypertension model Intraperitoneal injection 30 mg/kg Once daily for 28 days MK-886 reduced the development of chronic hypoxic pulmonary hypertension and right ventricular hypertrophy PMC507334

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.59mL

2.12mL

1.06mL

21.18mL

4.24mL

2.12mL

References

 

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