Zileuton (A-64077)

Catalog No.S1443 Synonyms: Abbott 64077, ZYFLO

For research use only.

Zileuton (A-64077, Abbott 64077, ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.

Zileuton (A-64077) Chemical Structure

CAS No. 111406-87-2

Selleck's Zileuton (A-64077) has been cited by 4 Publications

1 Customer Review

Purity & Quality Control

Choose Selective Lipoxygenase Inhibitors

Biological Activity

Description Zileuton (A-64077, Abbott 64077, ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.
Targets
Ferroptosis [6]
()
5-lipoxygenase [1]
()
In vitro

Zileuton suppresses PG biosynthesis by interference with arachidonic acid (AA) release in macrophages. Zileuton significantly reduces PGE2 and 6-keto prostaglandin F1α (PGF1α) levels in activated mouse peritoneal macrophages and in J774 macrophages. Zileuton inhibits PGE2 production in LPS-stimulated human whole blood and suppresses PGE2 and 6-keto PGF1α pleural levels in rat carrageenan-induced pleurisy. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RBI-1 NHfTb4hHfW6ldHnvckBie3OjeR?= NGHkNZJKdiC4aYTyc{BqdmirYnn0bY9vKG:oIEWtcIlxd3i7Z3XuZZNmKCh3LXzvLUBnem:vIITo[UAzODByMDDnJJN2eGW{bnH0ZY51KG:oIGLCTU0yKGOnbHzzMEBKSzVyPUCuOu69VQ>? MmrGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4Nkm4PUc,OjB4Nkm4PVww[T5?
RBL-1 NGHRfGdHfW6ldHnvckBie3OjeR?= NYrrWY9kUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgOU1tcXCxeInn[Y5ie2ViaX6gdoF1KFKETD2xJINmdGy|LDDJR|UxRTNwMt88US=> NIPP[Ws9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi96OEOxO|U6Lz56OEOxO|U6RC:jPh?=
basophilic leukemia cells NITzdINHfW6ldHnvckBie3OjeR?= MlXDTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JFUudGmyb4j5[4Vv[XOnIH;ieIFqdmWmIH\yc40hemG2IHLhd49xcGmuaXOgcIV2c2WvaXGgZ4VtdHNuIFnDOVA:OC53zszN NUC5WY1nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUS4OFQ6Oyd-OUS4OFQ6OzxxYU6=
RBL-2H3 MkPvSpVv[3Srb36gZZN{[Xl? MYjJcohq[mm2aX;uJI9nKDVvbHnwc5h6\2WwYYPlJI1m\GmjdHXkJINwdn[ncoPpc44hd2ZiW{G0R31iemGlaHnkc45q[yCjY3nkJJRwKGyndXvveJJq\W6nczDpckBTSkxvMlizJINmdGy|LDDJR|UxRTBwOEC0{txO MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86PTl7MkS2K|46PTl7MkS2QE9iRg>?
granulocytes-type cells NX3SeHZITnWwY4Tpc44h[XO|YYm= MmX4WIhmKGOxbYDveY5lKHejczDleoFtfWG2ZXSg[o9zKGm2czDpcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgOU1tcXCxeInn[Y5ie2VidYPpcoch\3KjboXsc4N6fGW|LYT5dIUh[2WubIOsJGlEPTB;Mj65{txO MlTvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF6NUmwNFEoRjFzOEW5NFAyRC:jPh?=
polymorphonuclear cells MlrFRY51cWyndXvveJJq\W6rYzDhd5NigQ>? NIrScYxCdnSrbHX1b491emmnbnnjJIFkfGm4aYT5JIlvKHKjdDDwc4x6dW:{cHjvcpVkdGWjcjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEyWQkSgZolwe3mwdHjld4l{NCCLQ{WwQVAvODIQvF2= Mly4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2NEi1O|UoRjF5NES4OVc2RC:jPh?=
MC9 NYPIOZpSTnWwY4Tpc44h[XO|YYm= NUG4c|YyUW6qaXLpeIlwdiCxZjDMWGI1KHC{b3T1Z5Rqd25iaX6gcY92e2ViTVO5JINmdGy|LDDJR|UxRTBwNUZOwG0> M4mxXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEm4NVUxLz5zOES5PFE2ODxxYU6=
MC9 MX;GeY5kfGmxbjDhd5NigQ>? M3jacGlvcGmkaYTpc44hd2ZibHX1b491emmnbnXzJJBzd2S3Y4Tpc44hcW5ibX;1d4UhVUN7IHPlcIx{ NFftOGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES5PFE2OCd-MUi0PVgyPTB:L3G+
PMNL MnXYSpVv[3Srb36gZZN{[Xl? NXW4cmZVOTVibXnudy=> MXTJcohq[mm2aX;uJI9nKDVvbHnwc5h6\2WwYYPlJIlvKGOnbHyg[pJm\SCVMUCwJIZz\XOqbImgbZNwdGG2ZXSgbJVu[W5iUF3OUEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFGyN|E5Py2|dHnteYxifGWmIEWtUG8heHKxZIXjeEBnd3KvYYTpc44heHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJI1m[XO3cnXkJIFnfGW{IEGwJI1qdnNiYomgTHBNSyCjbnHsfZNqeyxiSVO1NF0xNjYQvF2= MorTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUG2NlkoRjJ{NUWxOlI6RC:jPh?=
BMM MlnESpVv[3Srb36gZZN{[Xl? NULSOoR5OzBibXnudy=> M1LyeWlvcGmkaYTpc44hd2ZiNT3MU{BqdiCvb4Xz[UBDVU1iY3XscJMh[XO|ZYPz[YQh[XNiZn;ycYF1cW:wIH;mJGxVSzRiYX\0[ZIhOzBibXnud{BjgSCnbor5cYUhcW2vdX7vZZN{[XluIFnDOVA:OC5zOd88US=> MmDhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2M{K2NFUoRjJ4NEOyOlA2RC:jPh?=
A549 M32zcmZ2dmO2aX;uJIF{e2G7 MlXsNVUhdWmwcx?= MlTWTY5pcWKrdHnvckBw\iCvUFfFV{0yKGm|b3zheIVlKG[{b32gcYlkem:|b33ld{Bw\iCrboTldoxmfWurbj2xJIJmfGFvc4TpcZVt[XSnZDDoeY1idiCDNUS5JINmdGy|IIXzbY5oKFCJSEKgZZMhe3Wkc4TyZZRmKHC{ZXnuZ5Vj[XSnZDDmc5IhOTVibXnud{Bnd2yub4fl[EBjgSC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOSCvaX6gZpkhWlBvSGDMR{BidmGueYPpd{whUUN3ME2wMlbPxE1? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNEc,OzByNUO3NlA9N2F-
RAW264.7 MnvpSpVv[3Srb36gZZN{[Xl? NEjC[|U2KHWP M4e3[lI1KGi{cx?= Mme5TY5pcWKrdHnvckBw\iCOUGOvTWZP\2GvbXGtd5RqdXWuYYTl[EBtcXCrZDDw[ZJwgGmmYYTpc44hcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgZZQhPSC3TTDh[pRmeiB{NDDodpMh[nliQl;ETXB[KDV6MT:1PVEhSzFzLYP0ZYlvcW6pIHLhd4VlKE[DQ2OgZZN{[Xl? M3vDOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOU[0Nlk2Lz5|MEm2OFI6PTxxYU6=
RAW264.7 M2CxcmZ2dmO2aX;uJIF{e2G7 MU[1JJVO NUDDT2ZTPDhiaILz NWTBT4p5WHKxdHXjeIlwdiCjZ3HpcpN1KEySUz3pcoR2[2WmIHPlcIwh\GWjdHigbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[2WubDD2bYFjcWyrdImgZZQhPSC3TTDt[YF{fXKnZDDh[pRmeiB2ODDodpMh[nliTWTTJIF{e2G7IILlcIF1cX[nIITvJINwdnS{b3y= NFjtV4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm2OFI6PSd-M{C5OlQzQTV:L3G+
PMNL MUPGeY5kfGmxbjDhd5NigQ>? NUjEUm9UPSCvaX7z MojvTY5pcWKrdHnvckBw\iB3LVzPJIlvKGi3bXHuJHBOVkxiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIxmfWuxdILp[Y5mKG[xcn3heIlwdiCycnXpcoN2[mG2ZXSg[o9zKDVibXnud{Bnd2yub4fl[EBjgSC2aHHwd4lo[XKpaX6gd5RqdXWuYYTpc44hdWWjc4Xy[YQh[W[2ZYKgNVUhdWmwczDifUBTWC2KUFzDJIFv[Wy7c3nzMEBKSzVyPUKuN|HPxE1? M{TBVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMk[wPFg6Lz5|MUK2NFg5QTxxYU6=
HEK293 NYP0ZpRPTnWwY4Tpc44h[XO|YYm= MVuxJJVO NWDwV3Y3PSCvaX7z NXno[4tKUW6qaXLpeIlwdiCxZjDoeY1idiB3LVzPJJRz[W6|ZnXjeIVlKGmwIFjFT|I6OyClZXzsd{Bkd2W6cILld5NqdmdiRlzBVEBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gcIV2c2:2cnnlcoUh\m:{bXH0bY9vKGG2IEGgeW0hfXOrbnegZZJi[2irZH;ubYMh[WOrZDDhd{B{fWK|dILheIUheHKnaX7jeYJifGWmIH\vdkA2KG2rboOg[o9tdG:5ZXSgZpkh[2GuY3n1cUBqd26xcHjvdoUhSTJ|MUi3M4Fz[WOqaXTvcolkKGGlaXSgZYRlcXSrb36gZY5lKG2n NFHCfVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUK2NFg5QSd-M{GyOlA5QDl:L3G+
PMNL NXrvdotPTnWwY4Tpc44h[XO|YYm= M37PelEhfU1? NF\rNGo2KG2rboO= MX7Jcohq[mm2aX;uJI9nKDVvTF:gbY4hcHWvYX6gVG1PVCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gcIV2c2:2cnnlcoUh\m:{bXH0bY9vKGG2IEGgeW0heHKnaX7jeYJifGWmIH\vdkA2KG2rboOg[o9tdG:5ZXSgZpkhfGijcIPp[4Fz\2mwIIP0bY12dGG2aX;uJI1m[XO3cnXkJIFnfGW{IEG1JI1qdnNiYomgVnAuUFCOQzDhcoFtgXOrczDy[YxifGm4ZTD0c{Bkd262cn;s NVe2NYU1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GyOlA5QDlpPkOxNlYxQDh7PD;hQi=>
BL21 (DE3) NFL5ZWFHfW6ldHnvckBie3OjeR?= MWSxNEBucW6| NXO2SXJpUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjC1MYxqeG:6eXflcoF{\SCneIDy[ZN{\WRiaX6gSZNkcGW{aXPobYEh[2:uaTDCUFIyKCiGRUOpJINmdGy|IIXzbY5oKGG{YXPobYRwdmmlIHHjbYQh[XNic4Xid5Rz[XSnIIDy[Ylv[3WkYYTl[EBnd3JiMUCgcYlveyCob3zsc5dm\CCkeTDzeZNjfHKjdHWgZYRlcXSrb36gZY5lKG2nYYP1doVlKGGodHXyJFExKG2rboOgZpkhemW4ZYLz[UBxcGG|ZTDIVGxEKG2ndHjv[EwhUUN3ME2wMlXPxE1? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTR4NUKyOUc,OzF2NkWyNlU9N2F-
insect cells M4f5eGZ2dmO2aX;uJIF{e2G7 NH[3bGs2KG2rboO= M1PkVWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiNT3MU3gh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDwdo9lfWO2aX;uJI9nKDVvSGDFWGUh[W6mIEWtTGVVTSC3c3nu[{BiemGlaHnkc45q[yCjY3nkJIF{KHO3YoP0doF1\SCycnXpcoN2[mG2ZXSg[o9zKDVibXnud{Bnd2yub4fl[EBjgSC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOjBibXnud{BqdiCmYYLrJIJ6KG[ncoLpZ{BqdyxiSVO1NF0zOy57zszN NUTGbIJDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G3O|Q3PzZpPkOxO|c1Pjd4PD;hQi=>
RBL-2H3 Mn60SpVv[3Srb36gZZN{[Xl? NXvwSXlMUW6qaXLpeIlwdiCxZjC1MWxqeG:6eXflcoF{\SCxZjDyZZQh[mG|b4DobYxq[yCuZYXr[Y1q[SClZXzsd{whUUN3ME2wMlE1|ryP M4Drc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{Nyd-Q3jFUWJNRC:jPh?=
Sf21 M2fGRmZ2dmO2aX;uJIF{e2G7 M3noU|QhdWmwcx?= M1L4fGlvcGmkaYTpc44hd2ZicnH0JFUuVE:[IHX4dJJme3OnZDDpckBU\jJzIHnud4VkfCClZXzsd{BxemWrbnP1ZoF1\WRiZn;yJFQhdWmwczDmc4xtd3enZDDifUBCSSC|dXLzeJJifGViYXTkbZRqd25iYX7kJI1m[XO3cnXkJIFnfGW{IESgcYlveyCkeTDGU3gh[XO|YYmsJGlEPTB;MD6xPO69VQ>? NFr0[3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6Oy9pPlPoSW1DVDxxYU6=
RBL-2H3 MWXGeY5kfGmxbjDhd5NigQ>? MWPJckB3cXS{bzDpcohq[mm2aX;uJI9nKDVvbHnwc5h6\2WwYYPlJIlvKFKETD2yTFMhMFKjdDDiZZNweGirbHnjJIxmfWunbXnhLUBk\WyuczygTWM2OD1zLkK1{txO M3jzOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{Nyd-Q3jFUWJNRC:jPh?=
In vivo

Zileuton significantly reduces macroscopic damage score after four weeks of treatment in rats. Zileuton administration significantly increases the intracolonic release of both thromboxane B2 at week 1 and prostaglandin E2 at weeks 2 and 4 in rats. [2] Zileuton reduces the spinal cord inflammation and tissue injury, neutrophil infiltration, TNF-alpha, COX-2 and pERK1/2 expression, PGE(2) and LTB(4) production, and apoptosis in mice. Zileuton significantly improves the recovery of limb function over 10 days in mice.[3]

 

Zileuton administrated before I/R significantly reduces the degree of renal dysfunction (urea, creatinine) and injury (AST, histology) in 5-lipoxygenase knockout mice. Zileuton reduces the expression of ICAM-1 and the associated PMN infiltration caused by I/R of the mouse kidney in 5-lipoxygenase knockout mice. [4]

 

Zileuton inhibits LTB(4) production in the peritonitis model more effectively than the LTA(4)H inhibitor, but the influx of neutrophils into the peritoneum after 1 and 2 hours is significantly higher in Zileuton- versus JNJ-26993135-treated mice. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 47 mg/mL
(198.9 mM)
Water Insoluble
Ethanol '''47 mg/mL

Chemical Information

Molecular Weight 236.29
Formula

C11H12N2O2S

CAS No. 111406-87-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC2=CC=CC=C2S1)N(C(=O)N)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01136941 Completed Drug: Zileuton Sickle Cell Disease Children''s Hospital Medical Center Cincinnati September 2010 Phase 1
NCT01130688 Terminated Drug: Zileuton Chronic Myelogenous Leukemia University of Massachusetts Worcester January 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Zileuton (A-64077) | Zileuton (A-64077) supplier | purchase Zileuton (A-64077) | Zileuton (A-64077) cost | Zileuton (A-64077) manufacturer | order Zileuton (A-64077) | Zileuton (A-64077) distributor