Celecoxib 化学構造
分子量: 381.37

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製品説明

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    COX製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 セレコキシブは、40nMのIC50による選択的なCOX-2阻害剤です。
ターゲット COX-2
IC50 40 nM [1]
In vitro試験 Celecoxib shows low sensitivity against COX-1 with IC50 of 15 μM. [1] Celecoxib shows an anti-proliferative effect on nasopharyngeal carcinoma (NPC) cell lines including HNE1 and CNE1-LMP1 with IC50 of 32.86 μM and 61.31 μM, respectively. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
A549 MUTGeY5kfGmxbjDBd5NigQ>? NWXEZWx[OC5zLUOwJO69VQ>? NUSxWJFDPDhiaB?= NFftWHRqdmS3Y3XzJGlESU1vMTDlfJBz\XO|aX;uJI9vKGKxdHigdJJwfGWrbjDhcoQhdVKQQTDs[ZZmdA>? NWDrXZRmOjZ3MUOxO|I>
H460 M3rYNmZ2dmO2aX;uJGF{e2G7 MX:wMlEuOzBizszN MlLaOFghcA>? NFu5WYVqdmS3Y3XzJGlESU1vMTDlfJBz\XO|aX;uJI9vKGKxdHigdJJwfGWrbjDhcoQhdVKQQTDs[ZZmdA>? M{nle|I3PTF|MUey
HKESC-2 M13HUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXmNlDDqM7:TR?= MVe0POKhcMLi NVn0c2l[e2mpbnnmbYNidnSueTDpcoNz\WG|ZYOgeIhmKEmFNUFCpJZidHWnczDv[kBwgGGuaYDsZZRqdsLi MkXyNlY1PzR4OUO=
CaES-17 Mkn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnCenhmOjEEoN88US=> NWq4XY1VPDkEoHlCpC=> Mnvpd4lodmmoaXPhcpRtgSCrbnPy[YF{\XNidHjlJGlEPTEEoI\hcJVmeyCxZjDvfIFtcXCuYYTpcuKh NWKzeYw4OjZ2N{S2PVM>
HKESC-2 NVS5eHoySXCxcITvd4l{KEG|c3H5 MmrqNlDDqM7:TR?= M3XlN|Q5yqCqwrC= MkG1doVlfWOnczDvfIFtcXCuYYTpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> MUGyOlQ4PDZ7Mx?=
CaES-17 NET2WZJCeG:ydH;zbZMhSXO|YYm= MYKyNOKh|ryP MUG0POKhcMLi NHHHWGxz\WS3Y3XzJI95[WyrcHzheIlvNWmwZIXj[YQh[XCxcITvd4l{ M2LjeFI3PDd2Nkmz
A549 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLxZpk2NTF4MDFOwG0> NHnEfmk1QMLiaNMg M1rlTWROW09? NIO4PXZKSzVyPUG2N{41KM7:TR?= NICzXJAzPjR4NE[0Ny=>
HCC827 Ml7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXrOZI2NTF4MDFOwG0> NHfzXFA1QMLiaNMg NGfFS4FFVVOR NXjtXFhLUUN3ME22PU4zKM7:TR?= NX7xOWR[OjZ2NkS2OFM>
A549 NGToW5dCeG:ydH;zbZMhSXO|YYm= NGf5PWw5OCEEtV2= M4r5S|Q5yqCqwrC= M33HeWROW09? NX3vU2xtcW6mdXPld{BieG:ydH;zbZM> NF\mfGgzPjR4NE[0Ny=>
HCC827 M4O2ZmFxd3C2b4Ppd{BCe3OjeR?= MkXzPFAhyrWP NVTieGVZPDkEoHlCpC=> MXjEUXNQ NH\zXodqdmS3Y3XzJIFxd3C2b4Ppdy=> MXqyOlQ3PDZ2Mx?=
SGC-7901/DDP MVLGeY5kfGmxbjDBd5NigQ>? NWPUTFFWOTEEoNM1US=> NILpcJYzPCCq MXTpcohq[mm2czDjfYNtd2:6eXflcoF{\S1{IHHu[EBRNWeueXPvdJJwfGWrbjDlfJBz\XO|aX;u MlniNlY1ODd4NUO=
SGC-7901  MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCyOOKhcMLi M3Ti[mlEPTB;MUG1MlA5KM7:TR?= MYWyOlQxPzZ3Mx?=
SGC-7901/DDP MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jQPVI1yqCqwrC= MmjhTWM2OD1|NT60OUDPxE1? NEPQSZAzPjRyN{[1Ny=>
SGC-7901/DDP M3HRR2Fxd3C2b4Ppd{BCe3OjeR?= NVLJe49KOTEEoNM1US=> NFO2TFkzPCCq M{PCeYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhid3n0bEBkcXOybHH0bY4> NVHRc2Z1OjZ2MEe2OVM>
SGC-7901/DDP M3TYT2Z2dmO2aX;uJGF{e2G7 MWqxNOKhyrWP MYCyOEBp M3[3N4lvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJHAu\2y7Y3;wdo91\WmwIITodo92\2hiYnzvZ4tqdmdiRWCyMEBidmRiaX7hZ5RqfmG2aX7nJHBMSSCjbnSgR3JGSsLi M2DFV|I3PDB5NkWz
SGC-7901/DDP M1LzcGZ2dmO2aX;uJGF{e2G7 MXWxNOKhyrWP Mnu0NlQhcA>? NWLPcppW[2G3c3XzJIEhdWG{a3XkJIRm[3KnYYPlJIlvKHSqZTDs[ZZmdCCxZjDCZ4wuOiCycn;0[Ylv NFi1ZmYzPjRyN{[1Ny=>
H357 MkDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn4b4ZnPy53L{GwJO69VQ>? NEHRVIY1QCCq NYTrTnZKTE2VTx?= MUXpcohq[mm2czDj[YxtKGe{b4f0bOKh[2:vYnnu[YQhf2m2aDDTZYJ2fG:lbHH4 MlroNlYxODl6N{S=
TAF M1PjRWZ2dmO2aX;uJGF{e2G7 NEfJSIYyOMLiwsXN MXy3JIQ> NYnZV3ZX[W[oZXP0d{BVSU[|IHHkbIV{cX[nIIDyc5BmenSrZYO= NE\IZ2ozPTl6N{GyOy=>
TAF NEjVcYxHfW6ldHnvckBCe3OjeR?= MVKxNOKhyrWP NWrPSGNSOzBvMUKwJI1qdg>? NVTQV4g1eG:xcnz5JIFn\mWldIOg[GFsfCCyaH;zdIhwenmuYYTpc44h[2:wc3XxeYVvfCC2bzDFS2Yhe2mpbnHsbY5o NGHiPYYzPTl6N{GyOy=>
TAF NH\Qe4dHfW6ldHnvckBCe3OjeR?= MWSxNOKhyrWP MVW0PEBp NWLMXIE1cW6lcnXhd4V{KEWJRmKgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MViyOVk5PzF{Nx?=
PANC-1 NVfpb492T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XzclIxNzZyL{GwNEDPxE1? MYmyOE81QC95MjDo MkTxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NEHQZ2wzPTl5M{C2Ni=>
PANC-1 M2PROGZ2dmO2aX;uJGF{e2G7 MYmyNE83OC9zMECg{txO MYmyOEBp NXfKXJhu[XS2ZX71ZZR{KGOnbHygbY53[XOrb36gZY5lKG2rZ4LheIlwdiCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi NH;p[m0zPTl5M{C2Ni=>
HeLa  MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm4U5AzOMLizszNxsA> M3TNPFI1yqCq MUnlcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdg>? M3HLd|I2PzdyNEKz
SACC-83 NV3hS2R6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LN[VIxyqEQvF5CpC=> M1LGS|I1yqCq M{DxOYVvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:w M3H4d|I2PzdyNEKz
HeLa  MlP0RZBweHSxc3nzJGF{e2G7 NVXkVZh4OjEEoN88UeKh MYqyOOKhcA>? NF3y[mZmdmijbnPld{Bz[WSrYYTpc44ucW6mdXPl[EBqdmirYnn0bY9vKG:oIHPlcIwh[XCxcITvd4l{ MnH1NlU4PzB2MkO=
SACC-83 NEDWRmRCeG:ydH;zbZMhSXO|YYm= NXXiOW5NOjEEoN88UeKh MlK0NlTDqGh? NYT6TnRI\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQhcW6qaXLpeIlwdiCxZjDj[YxtKGGyb4D0c5Nqew>? M3HiXFI2PzdyNEKz
HeLa  M4XjVmZ2dmO2aX;uJGF{e2G7 NWfyeYw6OjBxNECvPFAh|ryP NUP0fIdpOjUEoHi= MkfWeZBz\We3bHH0d{BRXEWQIIDhdpRq[WyueTDifUBqdmirYnn0bY5oKFOyMTygZY5lKGGldHn2ZZRmeyCSVFXOJIFv\CCrbnHjeIl3[XSnczDBT3Q> M{fYR|I2PzdyNEKz
SACC-83 MVLGeY5kfGmxbjDBd5NigQ>? M2Dl[lIxNzRyL{iwJO69VQ>? M4PwfVI1yqCq M3zsV5VxemWpdXzheJMhWFSHTjDwZZJ1cWGubImgZpkhcW6qaXLpeIlv\yCVcEGsJIFv\CCjY4TpeoF1\XNiUGTFUkBidmRiaX7hZ5RqfmG2ZYOgRWtV M2W4R|I2PzdyNEKz
HLCZ01 NWrO[5hnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr0NQKBmzZywrFCuW0> M3jSRVQ5KGh? NIDrRmZFVVOR MYTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MmnlNlU4OjR6OUm=
HLCZ01 MW\GeY5kfGmxbjDBd5NigQ>? MVu0NOKh|ryP Mn:wNlQhcA>? NFfle|RFVVOR M2roWIlv[3KnYYPld{Bi[2O3bYXsZZRqd25ib3[gS|AwTzFvcHjhd4Uh[2WubIOgZ49u[mmwZXSge4l1cCCLRl6t{tE> NFHCRoMzPTd{NEi5PS=>
HLCZ01 NH\EUXdCeG:ydH;zbZMhSXO|YYm= NXjvTJZsPDEEoN88US=> Mli5NlQhcA>? Mn61SG1UVw>? Mn7n[Y5p[W6lZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiSV\OMe6y M3fiZ|I2PzJ2OEm5
HLCZ01 NYDYW3NbTnWwY4Tpc44hSXO|YYm= MoTnOFDDqM7:TR?= MVSyOEBp MkX0SG1UVw>? NUfLTmttcW6lcnXhd4V{KFSUQVnMJIV5eHKnc4Ppc44h[2:vYnnu[YQhf2m2aDDJcpRmem[ncn;uMe6y MnztNlU4OjR6OUm=
MGC803 NWWzTJBIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;WTVAuPjBizszN NXjkd21nPzJiaB?= Mn;jTWM2OD12Nz6yOgKBkcLz4pEJOk41OyEQvF2= MX6yOVcxOTN5OB?=
SGC7901 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnIboo{OC14MDFOwG0> MU[3NkBp M{[zSGlEPTB;NEOuOVPjiIoEsfMAjVUvOTJizszN MofFNlU4ODF|N{i=
MGC803 NIP3doJHfW6ldHnvckBCe3OjeR?= MY[0NOKh|ryP NH3lR3o5NzF4L{K0JIg> NHvMeYh2eHKnZ4XsZZR{KEOkbD3iJIV5eHKnc4Ppc44> NH[2TogzPTdyMUO3PC=>
SGC7901 M{G3PGZ2dmO2aX;uJGF{e2G7 MXW0NOKh|ryP NGnn[WU5NzF4L{K0JIg> MnTaeZBz\We3bHH0d{BE[mxvYjDlfJBz\XO|aX;u MUWyOVcxOTN5OB?=
MCF-7  NVvnRVRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\0NU8yOCEQvF2= M1r6bVczKGh? MmnoSG1UVw>? MV\lcohidmOnczDjZYxkcXS{aX;sMYlv\HWlZXSgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdg>? MXKyOVY3PzVzMB?=
MDA-MB-231  MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvPNU8yOCEQvF2= M{KwZVczKGh? MULEUXNQ MUXlcohidmOnczDjZYxkcXS{aX;sMYlv\HWlZXSgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdg>? MWmyOVY3PzVzMB?=
MDA-MB-231 MYXGeY5kfGmxbjDBd5NigQ>? MXKwMVQxKML3TR?= MnjEOE0zPCCq NWLMN2g6cW6lcnXhd4V{KEORWD2yJJBzd3SnaX6g[ZhxemW|c3nvckBqdiCkb4ToJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MXeyOVU5PzN{OR?=
MCF-7 MmPYSpVv[3Srb36gRZN{[Xl? NHHSRWsxNTRyINM1US=> MYC0MVI1KGh? NH;P[o9mdmijbnPld{B1cGViZX\m[YN1eyCxZjDUVGEhd25iQVLDS|Ih\XiycnXzd4lwdsLi MnLRNlU2QDd|Mkm=
MCF7-MX  M{HuUWZ2dmO2aX;uJGF{e2G7 NE\rNmsxNTRyINM1US=> M1TKb|QuOjRiaB?= NULmZVhy\W6qYX7j[ZMhfGinIHXm[oVkfHNib3[gWHBCKG:wIFHCR2czKGW6cILld5Nqd28EoB?= MXKyOVU5PzN{OR?=
MDA-MB-231 NELjOXpHfW6ldHnvckBCe3OjeR?= NUDwTpN3OC12MDFCuW0> NFrB[3o1NTJ2IHi= M{jZW5N1cW23bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhSUKFR{KgeZAhfG9iND6yO{B1cW2nczD0c{Bkd262cn;sJIxmfmWuIHL5JFEzKGkEoB?= Mnv2NlU2QDd|Mkm=
A2780 NXzobGxETnWwY4Tpc44hSXO|YYm= MkKyOU8yOC9zNTFOwG0> NEjkSFA1QCCq MX7k[YNz\WG|ZYOgR495NTJiZYjwdoV{e2mxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M4DTT|I2PDJ2OEm4
SKOV3  MmLiSpVv[3Srb36gRZN{[Xl? NGjxeI42NzFyL{G1JO69VQ>? NHvESZA1QCCq MUjk[YNz\WG|ZYOgR495NTJiZYjwdoV{e2mxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NF7sRnczPTR{NEi5PC=>
A2780 MofWSpVv[3Srb36gRZN{[Xl? M{j6V|UwOTBxMUWg{txO NYLBRpN3PDhiaB?= MnfT[YxmfmG2ZYOgeIhmKGW6cILld5Nqd25ib3[gSU1k[WSqZYLpckBidmRia3XyZZRqdg>? MmHPNlU1OjR6OUi=
SKOV3  M1fnSWZ2dmO2aX;uJGF{e2G7 M1;wSlUwOTBxMUWg{txO M2PhTVQ5KGh? M3HvSYVt\X[jdHXzJJRp\SCneIDy[ZN{cW:wIH;mJGUu[2GmaHXybY4h[W6mIHvldoF1cW5? M1L6Z|I2PDJ2OEm4
A2780 NWXuNHpQTnWwY4Tpc44hSXO|YYm= M2XLPVUwOTBxMUWg{txO M1jDbVQ5KGh? NFzUZmtl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhVi2lYXTo[ZJqdiCjbnSgWolu\W62aX6= NIrNWlIzPTR{NEi5PC=>
SKOV3  NYq0fnVOTnWwY4Tpc44hSXO|YYm= MV[1M|ExNzF3IN88US=> NH2z[|M1QCCq NYXQNmxQ\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKE5vY3HkbIVzcW5iYX7kJHZqdWWwdHnu MoLhNlU1OjR6OUi=
A2780 M4XIdmZ2dmO2aX;uJGF{e2G7 MleyOU8yOC9zNTFOwG0> NED1WpcyKGh? M3fDVYlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDv[kBxNUGNVDDhcoQheC2HUlugbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NX3vZpAyOjV2MkS4PVg>
SKOV3  NVnieJd{TnWwY4Tpc44hSXO|YYm= NUi0eWI5PS9zMD:xOUDPxE1? M4G1XFEhcA>? MWHpcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ib3[gdE1CU1RiYX7kJJAuTVKNIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M{TuVFI2PDJ2OEm4
HCT-15 NETaWpBHfW6ldHnvckBCe3OjeR?= NUfjPYw{OTBvNUCg{txO MUi2MVM3KGh? NHjUeJlqdmS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mJGNQYC1{IHnuJIJwfGhiZH;z[UBidmRidHnt[UBl\XCnbnTlcpQhdWGwbnXy NHXBTZQzPTJzOECyPC=>
HT-29  MXLGeY5kfGmxbjDBd5NigQ>? MWCxNE02OCEQvF2= NEjWU4M3NTN4IHi= NEn0UnNqdmS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mJGNQYC1{IHnuJIJwfGhiZH;z[UBidmRidHnt[UBl\XCnbnTlcpQhdWGwbnXy NV64enhyOjV{MUiwNlg>
HSC3  NV;pXY5OS2WubDDWbYFjcWyrdImgRZN{[Xl? NInQRowx6oDVNECg{txO NXTi[JJ[PDhiaB?= MVPJR|UxRTJ3LkZCtVEvPzhyIN88US=> NFHpbFczPTF7OEe4PS=>
HSC3  M3HKTGFxd3C2b4Ppd{BCe3OjeR?= NV\ESld7OjVizszN NICze3Q1QCCq NEjh[3BqdmS3Y3XzJIFxd3C2b4Ppdy=> NHTtZ5YzPTF7OEe4PS=>
HSC3  MnmwSpVv[3Srb36gRZN{[Xl? MX2yOUDPxE1? Ml7YOFghcA>? MWDlfIhq[mm2czDzbYdvcW[rY3HueIx6KHKnZIXj[YQhdWmpcnH0bY9vKGOxbXLpcoVlKHerdHigR2VV MoDTNlUyQTh5OEm=
HSC3  NXHrVJRPTnWwY4Tpc44hSXO|YYm= M4fmZlI2KM7:TR?= M2nhWlQ5KGh? NGHTellqdmirYnn0d{BJW0N|IHPlcIwhcW64YYPpc44h[2:vYnnu[YQhf2m2aDDDSXQ> NIOwUnUzPTF7OEe4PS=>
HSC3  NHrtdpdHfW6ldHnvckBCe3OjeR?= MYqyOUDPxE1? NWLET3plPzJiaB?= MUnk[YNz\WG|ZYOgUW1RNTJiYX7kJG1OWC17IIDyc5RmcW6|wrC= M2DGUVI2OTl6N{i5
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Hep-2 Mn:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOzNE82OC9zMECg{txO M3yxdFEzNzJ2L{O2M|Q5KGh? Ml[ySG1UVw>? M3;LXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MYKyOFk6QDV4NB?=
Hep-2 NV;3cI5ISXCxcITvd4l{KEG|c3H5 M13GZlUxKM7:TR?= NHrkR5cxNTR6IHi= NXnrVVU5TE2VTx?= MX3pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWg[IVx\W6mZX70JI1idm6nch?= NVX3eoZIOjR7OUi1OlQ>
Hep-2 NGrDT3FHfW6ldHnvckBCe3OjeR?= Mk\5OVAh|ryP NIC2OG0xNTR6IHi= NVn3N5dVTE2VTx?= M4f1TJJm\HWlZYOgeIhmKHSnbH;t[ZJie2ViYXP0bZZqfHliZ4Lh[JVidGy7 MX:yOFk6QDV4NB?=
Hep-2 NHPZT3hHfW6ldHnvckBCe3OjeR?= M371SlUxKM7:TR?= NGi3XGUxNTR6IHi= M1HLRmROW09? NEWyTZhl\WO{ZXHz[ZMhfGinIH3SUmEh\XiycnXzd4lwdiCxZjDoWGVTXA>? M1TkcFI1QTl6NU[0
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... Click to View More Cell Line Experimental Data

In vivo試験 Celecoxib exhibits a potent, oral anti-inflammatory activity. Celecoxib reduces acute inflammation in the carrageenan edema assay and chronic inflammation in the adjuvant arthritis model with ED50 of 7.1 mg/kg and 0.37 mg/kg/day, respectively. In addition, Celecoxib also exhibits analgesic activity in the Hargreaves hyperalgesia model with ED50 of 34.5 mg/kg. Besides, Celecoxib produces no acute GI toxicity in rats at doses up to 200 mg/kg and no chronic GI toxicity in rats at doses up to 600 mg/kg/day over 10 days. [1] In a C3Hf/KamLaw female mouse model, Celecoxib increases median survival time of 105 days (range, 79-145 days) after 13.5 Gy local thoracic irradiation (LTI) alone to 142 days (range, 94-155 days). [3]
臨床試験 Celecoxib is currently in Phase II clinical trials in patients with recurrent respiratory papillomatosis.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

COX enzyme assay in vitro Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation.

細胞アッセイ: [2]

細胞株 HNE1 and CNE1-LMP1
濃度 0-75 μM
反応時間 48 hours
実験の流れ The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 hours. The cells are then treated with increasing concentrations of Celecoxib (0 to 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 hours. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37 °C for 4 hours. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times.

動物実験: [1]

動物モデル A 0.1 mL aliquot of a 1% solution of carrageenan in 0.9% sterile saline or 1 mg of Mycobacterium butyricum in 50 μL of mineral oil is administered to the right hind foot pad of male Sprague−Dawley rats.
製剤 Celecoxib is dissolved in 0.5% methyl cellulose and 0.025% Tween-20.
投薬量 ≤200 mg/kg
投与方法 Administered via p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Celecoxib SDF
分子量 381.37
化学式

C17H14F3N3O2S

CAS No. 169590-42-5
保管 3年-20℃
2年-80℃in solvent
別名 SC 58635
溶解度 (25°C) * In vitro DMSO 76 mg/mL (199.28 mM)
Ethanol 33 mg/mL (86.53 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 4-(5-p-tolyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide

文献中の引用 (6)

Frequently Asked Questions

  • Question 1
    I am doing an animal experiment with mice and planning to administrate S1261 via oral gavage. what are your recommendations for diluting the compound?

    Answer: For oral administration, Celecoxib can be dissolved in vehicle one: "0.5% methyl cellulose and 0.025% Tween-20", or the vehicle 2 "2% DMSO/30% PEG 300/5% Tween 80/ ddH2O".

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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