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

Structure of MK-886
CAS No.: 118414-82-7

Chemical Structure| 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

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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 References
Jurkat cells 200 nM 30 minutes Inhibit LTB4 secretion and reduce Jurkat cell migration Nat Commun. 2017 Jun 22;8:15890.
C91/PL cells 200 nM 30 minutes Inhibit LTB4 secretion and reduce contact formation with Jurkat cells Nat Commun. 2017 Jun 22;8:15890.
Rat pulmonary vascular endothelial cells 10^-5 M 10 minutes MK-886 significantly reduced the pressor responses induced by angiotensin II and hypoxia J Clin Invest. 1996 Jun 1;97(11):2491-8.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
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. Nat Commun. 2016 Feb 23;7:10760.
Humanized mice HTLV-1 infection model Intraperitoneal injection 5 nmol Three times a week for six weeks To evaluate the effect of MK886 treatment on LTB4 plasma levels and viral load in HTLV-1-infected mice. Results showed that MK886 treatment significantly reduced LTB4 plasma levels and viral load. Nat Commun. 2017 Jun 22;8:15890.
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 Nat Neurosci. 2010 Oct;13(10):1265-70
Rats Chronic hypoxic pulmonary hypertension model Intraperitoneal injection 30 mg/kg Once daily for 28 days MK-886 inhibited the development of chronic hypoxic pulmonary hypertension, reducing pulmonary artery pressure and right ventricular hypertrophy J Clin Invest. 1996 Jun 1;97(11):2491-8.
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 Nat Commun. 2017 Jun 22;8:15890.
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 J Clin Invest. 1996 Jun 1;97(11):2491-8.
Mice Zymosan-induced peritonitis Intraperitoneal injection 1 mg/kg Single dose, 30 minutes prior Evaluate the effect of MK886 on reducing LTB4 levels, showing more significant effects in female mice J Clin Invest. 2017 Aug 1;127(8):3167-3176

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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