MK-886 (Synonyms: L 663536)

Name: MK-886
Brand: MedChemExpress
SKU: HY-14166
Rating: 5.0 (13 reviews)

Cat. No.: HY-14166 Purity: 99.13%: Data Sheet
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MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC₅₀ of 30 nM) and leukotriene biosynthesis (IC₅₀s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.

For research use only. We do not sell to patients.

CAS No. : 118414-82-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of MK-886:

MK-886 sodium salt Get quote
MK-886 (Standard) Get quote

13 Publications Citing Use of MCE MK-886

In Vivo Efficacy Study

Histological Imaging/Staining

RT-PCR

: MK-886 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Jun:62:102706. [Abstract]; Male mice were pretreated with MK-886 (20 mg/kg) and epoxomicin (Epox, 1 mg/kg) at 2 and 24 h before I/R-mediated cardiac injury. Echocardiographic images of the left ventricle (left). Scale bar: 0.2 s. Quantification of EF% and FS% (right, n = 6).

: MK-886 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Jun:62:102706. [Abstract]; Male mice were pretreated with MK-886 (20 mg/kg) and epoxomicin (Epox, 1 mg/kg) at 2 and 24 h before I/R-mediated cardiac injury. Images of Evans blue and TTC staining (left) for infarct size analysis, with quantification of the infarction area/left ventricular (LV) area and area at risk (AAR)/LV area ratios (right; n = 6).

: MK-886 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Jun:62:102706. [Abstract]; Male mice were pretreated with MK-886 (20 mg/kg) and epoxomicin (Epox, 1 mg/kg) at 2 and 24 h before I/R-mediated cardiac injury. Images of TUNEL (red), α-actinin (green), and DAPI (blue) staining of cardiac slices (left) and the percentage of TUNEL+ nuclei (right; n = 6).

: MK-886 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2023 Jun:62:102706. [Abstract]; Male mice were pretreated with MK-886 (20 mg/kg) and epoxomicin (Epox, 1 mg/kg) at 2 and 24 h before I/R-mediated cardiac injury. qPCR analysis of Bax and Bcl-2 mRNA levels in the border zone of the ischemic heart (n = 6) and quantification of the relative Bax/Bcl-2 ratio.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 30 nM (FLAP)^[3]
IC50: 3 nM (Leukotriene biosynthesis in intact leukocytes) and 1.1 μM (Leukotriene biosynthesis in human whole blood)^[2]
PPARα^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2 3 Compound: MK-886	Inhibition of PGES-1 in human A549 cell microsomes using PGH2 as substrate assessed as suppression of interleukin-1beta-stimulated PGE2 production incubated for 15 mins post interleukin-1beta challenge for 72 hrs by RP-HPLC analysis Inhibition of PGES-1 in human A549 cell microsomes using PGH2 as substrate assessed as suppression of interleukin-1beta-stimulated PGE2 production incubated for 15 mins post interleukin-1beta challenge for 72 hrs by RP-HPLC analysis	[PMID: 26602278]
A549	IC₅₀	2.5 3 Compound: MK886	Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis	[PMID: 28240894]
A549	IC₅₀	2.1 3 Compound: MK-886	Inhibition of mPGES1 in IL-1beta treated human A549 cell microsomal membrane assessed as inhibition of PGE2 formation incubated for 15 mins before addition of PGH2 by RP-HPLC method Inhibition of mPGES1 in IL-1beta treated human A549 cell microsomal membrane assessed as inhibition of PGE2 formation incubated for 15 mins before addition of PGH2 by RP-HPLC method	[PMID: 21800856]
A549	IC₅₀	2.4 3 Compound: MK-886	Inhibition of microsomal PGES1 isolated from IL-1beta-stimulated human A549 cells preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis Inhibition of microsomal PGES1 isolated from IL-1beta-stimulated human A549 cells preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis	[PMID: 24844534]
A549	IC₅₀	3 3 Compound: MK-886	Inhibition of mPGES-1 expressed in LPS-stimulated human A549 cells mitochondrial fraction assessed as conversion of PGH2 to PGE2 Inhibition of mPGES-1 expressed in LPS-stimulated human A549 cells mitochondrial fraction assessed as conversion of PGH2 to PGE2	[PMID: 21310608]
A549	IC₅₀	2.1 3 Compound: MK-886	Inhibition of PGES-1 in IL-1beta stimulated human A549 cell microsomes using PGH2 as substrate assessed as suppression of PGE2 formation preincubated for 15 mins followed by substrate addition by reversed phase-HPLC analysis Inhibition of PGES-1 in IL-1beta stimulated human A549 cell microsomes using PGH2 as substrate assessed as suppression of PGE2 formation preincubated for 15 mins followed by substrate addition by reversed phase-HPLC analysis	[PMID: 26777299]
A549	IC₅₀	2.1 3 Compound: 9, MK-886	Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay	[PMID: 19053751]
A549	IC₅₀	2.4 3 Compound: 33, MK-886	Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis	[PMID: 24171493]
A549	IC₅₀	2.3 3 Compound: MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis	[PMID: 22992107]
A549	IC₅₀	2.11 3 Compound: 1, MK-886	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method	[PMID: 19719242]
A549	IC₅₀	2.2 3 Compound: 31, MK886	Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method	[PMID: 25765759]
A549	IC₅₀	2.4 3 Compound: 26, MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins	[PMID: 21570310]
A549	IC₅₀	2.4 3 Compound: 36, MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis	[PMID: 21591611]
A549	IC₅₀	2.3 3 Compound: MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis	[PMID: 22992107]
A549	IC₅₀	2 3 Compound: 1	Inhibition of mPGES1 in IL1-beta induced human A549 cell microsomal membrane assessed as blockade of conversion of PGH2 to PGE2 Inhibition of mPGES1 in IL1-beta induced human A549 cell microsomal membrane assessed as blockade of conversion of PGH2 to PGE2	[PMID: 19884011]
A549	IC₅₀	2.4 3 Compound: 33, MK-886	Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis	[PMID: 24171493]
A549	IC₅₀	2 3 Compound: 1	Inhibition of mPGES1 in IL1-beta induced human A549 cell microsomal membrane assessed as blockade of conversion of PGH2 to PGE2 Inhibition of mPGES1 in IL1-beta induced human A549 cell microsomal membrane assessed as blockade of conversion of PGH2 to PGE2	[PMID: 19884011]
A549	IC₅₀	2 3 Compound: MK-886	Inhibition of PGES-1 in human A549 cell microsomes using PGH2 as substrate assessed as suppression of interleukin-1beta-stimulated PGE2 production incubated for 15 mins post interleukin-1beta challenge for 72 hrs by RP-HPLC analysis Inhibition of PGES-1 in human A549 cell microsomes using PGH2 as substrate assessed as suppression of interleukin-1beta-stimulated PGE2 production incubated for 15 mins post interleukin-1beta challenge for 72 hrs by RP-HPLC analysis	[PMID: 26602278]
A549	IC₅₀	2.4 3 Compound: MK-886	Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method	[PMID: 26088337]
A549	IC₅₀	2.2 3 Compound: 31, MK886	Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method	[PMID: 25765759]
A549	IC₅₀	2.1 3 Compound: 9, MK-886	Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay	[PMID: 19053751]
A549	IC₅₀	2.4 3 Compound: 36, MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis	[PMID: 21591611]
A549	IC₅₀	2.1 3 Compound: MK-886	Inhibition of mPGES1 in IL-1beta treated human A549 cell microsomal membrane assessed as inhibition of PGE2 formation incubated for 15 mins before addition of PGH2 by RP-HPLC method Inhibition of mPGES1 in IL-1beta treated human A549 cell microsomal membrane assessed as inhibition of PGE2 formation incubated for 15 mins before addition of PGH2 by RP-HPLC method	[PMID: 21800856]
A549	IC₅₀	2.11 3 Compound: 1, MK-886	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method	[PMID: 19719242]
A549	IC₅₀	2.4 3 Compound: MK-886	Inhibition of microsomal PGES1 isolated from IL-1beta-stimulated human A549 cells preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis Inhibition of microsomal PGES1 isolated from IL-1beta-stimulated human A549 cells preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis	[PMID: 24844534]
A549	IC₅₀	2.1 3 Compound: MK-886	Inhibition of mPGES1 in IL-1beta treated human A549 cell microsomal membrane assessed as inhibition of PGE2 formation incubated for 15 mins before addition of PGH2 by RP-HPLC method Inhibition of mPGES1 in IL-1beta treated human A549 cell microsomal membrane assessed as inhibition of PGE2 formation incubated for 15 mins before addition of PGH2 by RP-HPLC method	[PMID: 21800856]
A549	IC₅₀	2.4 3 Compound: 26, MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins	[PMID: 21570310]
A549	IC₅₀	2.4 3 Compound: MK-886	Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method	[PMID: 26088337]
A549	IC₅₀	2.1 3 Compound: MK-886	Inhibition of PGES-1 in IL-1beta stimulated human A549 cell microsomes using PGH2 as substrate assessed as suppression of PGE2 formation preincubated for 15 mins followed by substrate addition by reversed phase-HPLC analysis Inhibition of PGES-1 in IL-1beta stimulated human A549 cell microsomes using PGH2 as substrate assessed as suppression of PGE2 formation preincubated for 15 mins followed by substrate addition by reversed phase-HPLC analysis	[PMID: 26777299]
A549	IC₅₀	2.11 3 Compound: 1, MK-886	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method	[PMID: 19719242]
A549	IC₅₀	2.5 3 Compound: MK886	Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis	[PMID: 28240894]
A549	IC₅₀	2.7 3 Compound: MK-886	Inhibition of mPGES-1 in interleukin-1 beta-stimulated human A549 cells microsomal membranes assessed as reduction in conversion of PGH2 to PGE2 pre-incubated for 15 mins followed by PGH2 substrate addition measured after 1 min by RP-HPLC method Inhibition of mPGES-1 in interleukin-1 beta-stimulated human A549 cells microsomal membranes assessed as reduction in conversion of PGH2 to PGE2 pre-incubated for 15 mins followed by PGH2 substrate addition measured after 1 min by RP-HPLC method	[PMID: 28165233]
A549	IC₅₀	2.2 3 Compound: 31, MK886	Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method	[PMID: 25765759]
A549	IC₅₀	2.1 3 Compound: 9, MK-886	Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay	[PMID: 19053751]
A549	IC₅₀	2.7 3 Compound: MK-886	Inhibition of mPGES-1 in interleukin-1 beta-stimulated human A549 cells microsomal membranes assessed as reduction in conversion of PGH2 to PGE2 pre-incubated for 15 mins followed by PGH2 substrate addition measured after 1 min by RP-HPLC method Inhibition of mPGES-1 in interleukin-1 beta-stimulated human A549 cells microsomal membranes assessed as reduction in conversion of PGH2 to PGE2 pre-incubated for 15 mins followed by PGH2 substrate addition measured after 1 min by RP-HPLC method	[PMID: 28165233]
A549	IC₅₀	2 3 Compound: MK-886	Inhibition of PGES-1 in human A549 cell microsomes using PGH2 as substrate assessed as suppression of interleukin-1beta-stimulated PGE2 production incubated for 15 mins post interleukin-1beta challenge for 72 hrs by RP-HPLC analysis Inhibition of PGES-1 in human A549 cell microsomes using PGH2 as substrate assessed as suppression of interleukin-1beta-stimulated PGE2 production incubated for 15 mins post interleukin-1beta challenge for 72 hrs by RP-HPLC analysis	[PMID: 26602278]
A549	IC₅₀	2.3 3 Compound: MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis	[PMID: 22992107]
CHO-K1	IC₅₀	8.2 3 Compound: 1, Mk-886	Inhibition of rat mPGES-1 transfected in CHOK1 cells using [3H]PGH2 as substrate Inhibition of rat mPGES-1 transfected in CHOK1 cells using [3H]PGH2 as substrate	[PMID: 23266122]
A549	IC₅₀	2.1 3 Compound: MK-886	Inhibition of PGES-1 in IL-1beta stimulated human A549 cell microsomes using PGH2 as substrate assessed as suppression of PGE2 formation preincubated for 15 mins followed by substrate addition by reversed phase-HPLC analysis Inhibition of PGES-1 in IL-1beta stimulated human A549 cell microsomes using PGH2 as substrate assessed as suppression of PGE2 formation preincubated for 15 mins followed by substrate addition by reversed phase-HPLC analysis	[PMID: 26777299]
A549	IC₅₀	2.4 3 Compound: 26, MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins	[PMID: 21570310]
CHO	IC₅₀	1.6 3 Compound: 13	Inhibition of human recombinant mPGES1 expressed in CHO cells Inhibition of human recombinant mPGES1 expressed in CHO cells	[PMID: 18459759]
A549	IC₅₀	2.4 3 Compound: 33, MK-886	Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis	[PMID: 24171493]
CHO-K1	IC₅₀	8.2 3 Compound: 1, Mk-886	Inhibition of rat mPGES-1 transfected in CHOK1 cells using [3H]PGH2 as substrate Inhibition of rat mPGES-1 transfected in CHOK1 cells using [3H]PGH2 as substrate	[PMID: 23266122]
A549	IC₅₀	2.4 3 Compound: 36, MK-886	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis	[PMID: 21591611]
A549	IC₅₀	2.4 3 Compound: MK-886	Inhibition of microsomal PGES1 isolated from IL-1beta-stimulated human A549 cells preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis Inhibition of microsomal PGES1 isolated from IL-1beta-stimulated human A549 cells preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis	[PMID: 24844534]
RBL-2H3	IC₅₀	5 1 Compound: MK-886	The compound was tested for inhibitory activity against 5-lipoxygenase translocation inhibitor in rat RBL-2H3 cells The compound was tested for inhibitory activity against 5-lipoxygenase translocation inhibitor in rat RBL-2H3 cells	[PMID: 1635053]
A549	IC₅₀	2.4 3 Compound: MK-886	Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method	[PMID: 26088337]
PMNL	IC₅₀	0.09 3 Compound: 9, MK-886	Inhibition of 5-LO in PMNL cells Inhibition of 5-LO in PMNL cells	[PMID: 19053751]
A549	IC₅₀	2.5 3 Compound: MK886	Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis	[PMID: 28240894]
A549	IC₅₀	2.7 3 Compound: MK-886	Inhibition of mPGES-1 in interleukin-1 beta-stimulated human A549 cells microsomal membranes assessed as reduction in conversion of PGH2 to PGE2 pre-incubated for 15 mins followed by PGH2 substrate addition measured after 1 min by RP-HPLC method Inhibition of mPGES-1 in interleukin-1 beta-stimulated human A549 cells microsomal membranes assessed as reduction in conversion of PGH2 to PGE2 pre-incubated for 15 mins followed by PGH2 substrate addition measured after 1 min by RP-HPLC method	[PMID: 28165233]
A549	IC₅₀	3 3 Compound: MK-886	Inhibition of mPGES-1 expressed in LPS-stimulated human A549 cells mitochondrial fraction assessed as conversion of PGH2 to PGE2 Inhibition of mPGES-1 expressed in LPS-stimulated human A549 cells mitochondrial fraction assessed as conversion of PGH2 to PGE2	[PMID: 21310608]
CHO	IC₅₀	1.6 3 Compound: 13	Inhibition of human recombinant mPGES1 expressed in CHO cells Inhibition of human recombinant mPGES1 expressed in CHO cells	[PMID: 18459759]
CHO-K1	IC₅₀	8.2 3 Compound: 1, Mk-886	Inhibition of rat mPGES-1 transfected in CHOK1 cells using [3H]PGH2 as substrate Inhibition of rat mPGES-1 transfected in CHOK1 cells using [3H]PGH2 as substrate	[PMID: 23266122]
PMNL	IC₅₀	0.09 3 Compound: 9, MK-886	Inhibition of 5-LO in PMNL cells Inhibition of 5-LO in PMNL cells	[PMID: 19053751]
RBL-2H3	IC₅₀	5 1 Compound: MK-886	The compound was tested for inhibitory activity against 5-lipoxygenase translocation inhibitor in rat RBL-2H3 cells The compound was tested for inhibitory activity against 5-lipoxygenase translocation inhibitor in rat RBL-2H3 cells	[PMID: 1635053]

In Vitro

MK-886 (0.5-2 μM; 15 hours; primary keratinocytes) treatment reduces keratin-1 expression in a culture of mouse primary keratinocytes^[1].
Using a transient transfection system in monkey kidney fibroblast CV-1 cells, mouse keratinocyte 308 cells and human lung adenocarcinoma A549 cells, 10 μM MK-886 is able to inhibit Wy-14643 activation of PPARα by ~80%. MK-886 also decreases PPARα activation by fatty acids in the stable transfection system^[1].
Although Jurkat cells express all PPAR isoforms, various PPARα and PPARγ agonists are unable to prevent MK-886-induced apoptosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	Primary keratinocytes
Concentration:	0.5 µM, 1 µM or 2 µM
Incubation Time:	15 hours
Result:	Decreased in keratin-1 expression.

In Vivo

MK-886 (L 663536; 5 mg/kg; oral administration; male Sprague-Dawley rats) treatment potently inhibits the antigen-induced dyspnea in inbred rats pretreated with methysergide^[2].
MK-886 (L 663536) inhibits leukotriene biosynthesis in vivo in a rat pleurisy model (ED₅₀, 0.2 mg/kg p.o.), an inflamed rat paw model (ED₅₀, 0.8 mg/kg), a model of leukotriene excretion in rat bile following antigen provocation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats (300-400 g) with antigen-induced dyspnea^[1]
Dosage:	5 mg/kg
Administration:	Oral administration
Result:	Inhibited the antigen-induced dyspnea.

Molecular Weight

472.08

Formula

C₂₇H₃₄ClNO₂S

CAS No.

118414-82-7

Appearance

Solid

Color

White to off-white

SMILES

CC(C)C1=CC=C(N(CC2=CC=C(Cl)C=C2)C(CC(C)(C(O)=O)C)=C3SC(C)(C)C)C3=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 75 mg/mL (158.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1183 mL	10.5914 mL	21.1828 mL
5 mM	0.4237 mL	2.1183 mL	4.2366 mL
10 mM	0.2118 mL	1.0591 mL	2.1183 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.30 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (4.41 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.08 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (21.18 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (284 KB) SDS (254 KB)

COA (257 KB) HNMR (254 KB) RP-HPLC (257 KB) MS (104 KB)

Handling Instructions (2659 KB)

References

[1]. Kehrer JP et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochem J. 2001 Jun 15. [Content Brief]

[2]. Gillard J et al. L-663,536 (MK-886) (3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2 - dimethylpropanoic acid), a novel, orally active leukotriene biosynthesis inhibitor. Can J Physiol Pharmacol. 1989 May;67(5):456-64. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1183 mL	10.5914 mL	21.1829 mL	52.9571 mL
	5 mM	0.4237 mL	2.1183 mL	4.2366 mL	10.5914 mL
	10 mM	0.2118 mL	1.0591 mL	2.1183 mL	5.2957 mL
	15 mM	0.1412 mL	0.7061 mL	1.4122 mL	3.5305 mL
	20 mM	0.1059 mL	0.5296 mL	1.0591 mL	2.6479 mL
	25 mM	0.0847 mL	0.4237 mL	0.8473 mL	2.1183 mL
	30 mM	0.0706 mL	0.3530 mL	0.7061 mL	1.7652 mL
	40 mM	0.0530 mL	0.2648 mL	0.5296 mL	1.3239 mL
	50 mM	0.0424 mL	0.2118 mL	0.4237 mL	1.0591 mL
	60 mM	0.0353 mL	0.1765 mL	0.3530 mL	0.8826 mL
	80 mM	0.0265 mL	0.1324 mL	0.2648 mL	0.6620 mL
	100 mM	0.0212 mL	0.1059 mL	0.2118 mL	0.5296 mL

MK-886 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MK-886 (Synonyms: L 663536)

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13 Publications Citing Use of MCE MK-886

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MK-886 (Synonyms: L 663536)

Customer Review

Other Forms of MK-886:

MK-886 Related Antibodies

13 Publications Citing Use of MCE MK-886

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Leukotriene Receptor Isoform Specific Products:

View All PPAR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

MK-886 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

MK-886 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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SAFETY DATA SHEET (SDS)

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