Celecoxib 化学構造
分子量: 381.37

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製品説明

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  • 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 MnnnSpVv[3Srb36gRZN{[Xl? NH\rV2YxNjFvM{Cg{txO NFfIXIE1QCCq M1zhO4lv\HWlZYOgTWNCVS1zIHX4dJJme3Orb36gc44h[m:2aDDwdo91\WmwIHHu[EBuWk6DIHzleoVt M3jNOVI3PTF|MUey
H460 NX\4O5lQTnWwY4Tpc44hSXO|YYm= MUKwMlEuOzBizszN NXfETHNVPDhiaB?= MVHpcoR2[2W|IFnDRW0uOSCneIDy[ZN{cW:wIH;uJIJwfGhicILveIVqdiCjbnSgcXJPSSCuZY\lcC=> NXrRRm1bOjZ3MUOxO|I>
HKESC-2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T1VFIxyqEQvF2= NYPnU2tLPDkEoHlCpC=> MmTld4lodmmoaXPhcpRtgSCrbnPy[YF{\XNidHjlJGlEPTEEoI\hcJVmeyCxZjDvfIFtcXCuYYTpcuKh MXyyOlQ4PDZ7Mx?=
CaES-17 M3SzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[yNOKh|ryP NWfOdodkPDkEoHlCpC=> M2PXZpNq\26rZnnjZY51dHliaX7jdoVie2W|IITo[UBKSzVywrD2ZYx2\XNib3[gc5hidGmybHH0bY7DqA>? M13rcVI3PDd2Nkmz
HKESC-2 MlzNRZBweHSxc3nzJGF{e2G7 NULoNY9ZOjEEoN88US=> NE\ITJE1QMLiaNMg NUTH[o5FemWmdXPld{BwgGGuaYDsZZRqdi2rbnT1Z4VlKGGyb4D0c5Nqew>? NX\IboMxOjZ2N{S2PVM>
CaES-17 NVe5PYY4SXCxcITvd4l{KEG|c3H5 NITMPGQzOMLizszN MYq0POKhcMLi M2LuWpJm\HWlZYOgc5hidGmybHH0bY4ucW6mdXPl[EBieG:ydH;zbZM> NWjtfnpTOjZ2N{S2PVM>
A549 M2PaOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TkVlUuOTZyIN88US=> NFzHUHY1QMLiaNMg NEfobWtFVVOR NVXabY5sUUN3ME2xOlMvPCEQvF2= MUeyOlQ3PDZ2Mx?=
HCC827 NGHPW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLHWVl6PS1zNkCg{txO M2TIXFQ5yqCqwrC= NEfzellFVVOR M1jyfGlEPTB;NkmuNkDPxE1? MlT5NlY1PjR4NEO=
A549 MVXBdI9xfG:|aYOgRZN{[Xl? Mlv1PFAhyrWP MoC5OFjDqGkEoB?= M37jWGROW09? NGLjdZdqdmS3Y3XzJIFxd3C2b4Ppdy=> NWO0XXFnOjZ2NkS2OFM>
HCC827 MlT4RZBweHSxc3nzJGF{e2G7 NFHqVWU5OCEEtV2= MojPOFjDqGkEoB?= M4HMVmROW09? NVr0dFJEcW6mdXPld{BieG:ydH;zbZM> Ml2wNlY1PjR4NEO=
SGC-7901/DDP M1\tdWZ2dmO2aX;uJGF{e2G7 MmfaNVDDqML3TR?= NXvsbWVkOjRiaB?= NH7ITHpqdmirYnn0d{BkgWOub3;4fYdmdmG|ZT2yJIFv\CCSLXfsfYNweHKxdHXpckBmgHC{ZYPzbY9v MkSxNlY1ODd4NUO=
SGC-7901  MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrHNlTDqGkEoB?= NYWyOVhtUUN3ME2xNVUvODhizszN NV\uZ3Q4OjZ2MEe2OVM>
SGC-7901/DDP M4HmU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqyOOKhcMLi MWXJR|UxRTN3LkS1JO69VQ>? MXuyOlQxPzZ3Mx?=
SGC-7901/DDP M4PWPGFxd3C2b4Ppd{BCe3OjeR?= NU\rNFk{OTEEoNM1US=> MlnWNlQhcA>? NYD0WpRFcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDD3bZRpKGOrc4DsZZRqdg>? MnHlNlY1ODd4NUO=
SGC-7901/DDP NWjW[2dUTnWwY4Tpc44hSXO|YYm= NIOwTZcyOMLiwsXN M3\0O|I1KGh? M4ntZYlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJHAu\2y7Y3;wdo91\WmwIITodo92\2hiYnzvZ4tqdmdiRWCyMEBidmRiaX7hZ5RqfmG2aX7nJHBMSSCjbnSgR3JGSsLi Ml2yNlY1ODd4NUO=
SGC-7901/DDP MnjSSpVv[3Srb36gRZN{[Xl? NUHqWlA6OTEEoNM1US=> MXqyOEBp NH72O2hk[XW|ZYOgZUBu[XKtZXSg[IVkemWjc3WgbY4hfGinIHzleoVtKG:oIFLjcE0zKHC{b4TlbY4> NH\EPYwzPjRyN{[1Ny=>
H357 MnjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXneYtiPy53L{GwJO69VQ>? M3S0e|Q5KGh? MkW1SG1UVw>? NEDrVJlqdmirYnn0d{Bk\WyuIHfyc5d1cMLiY3;tZolv\WRid3n0bEBU[WK3dH;jcIF5 NF3QdHAzPjByOUi3OC=>
TAF NXv3WYRHTnWwY4Tpc44hSXO|YYm= M1zKTFExyqEEtV2= NF7pXog4KGR? MlrlZYZn\WO2czDURWZ{KGGmaHXzbZZmKHC{b4DldpRq\XN? MXeyOVk5PzF{Nx?=
TAF NVHqe5h5TnWwY4Tpc44hSXO|YYm= MXqxNOKhyrWP MVqzNE0yOjBibXnu NI\Gb3pxd2:{bImgZYZn\WO2czDkRYt1KHCqb4PwbI9zgWyjdHnvckBkd26|ZYH1[Y51KHSxIFXHSkB{cWewYXzpcoc> Mn7WNlU6QDdzMke=
TAF M4fETGZ2dmO2aX;uJGF{e2G7 NVj1SVFoOTEEoNM1US=> NY\STpBrPDhiaB?= NEe1TWVqdmO{ZXHz[ZMhTUeIUjDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= MmnXNlU6QDdzMke=
PANC-1 M1q2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWGy[pQ2OjBxNkCvNVAxKM7:TR?= Mkf0NlQwPDhxN{KgbC=> MmLsbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXuyOVk4OzB4Mh?=
PANC-1 M3nRXWZ2dmO2aX;uJGF{e2G7 NEG3XlgzOC94MD:xNFAh|ryP NF\XXmczPCCq NGXaUYxifHSnboXheJMh[2WubDDpcpZie2mxbjDhcoQhdWmpcnH0bY9vKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzyqB? MWmyOVk4OzB4Mh?=
HeLa  MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqyNOKh|ryPwrC= NYHlfpc3OjUEoHi= MlLn[Y5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25? MVOyOVc4ODR{Mx?=
SACC-83 M2Dl[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nueVIxyqEQvF5CpC=> MX6yOOKhcA>? M3PSeYVvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:w M3;EflI2PzdyNEKz
HeLa  NGDMbphCeG:ydH;zbZMhSXO|YYm= NWHYSnlTOjEEoN88UeKh NXfVfFVFOjUEoHi= NV;3SplT\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQhcW6qaXLpeIlwdiCxZjDj[YxtKGGyb4D0c5Nqew>? NYPXXGVuOjV5N{C0NlM>
SACC-83 NVTCcmp4SXCxcITvd4l{KEG|c3H5 M3fiRlIxyqEQvF5CpC=> NXuyTZJXOjUEoHi= NGHMRlZmdmijbnPld{Bz[WSrYYTpc44ucW6mdXPl[EBqdmirYnn0bY9vKG:oIHPlcIwh[XCxcITvd4l{ MmqzNlU4PzB2MkO=
HeLa  M1nHb2Z2dmO2aX;uJGF{e2G7 Ml3RNlAwPDBxOECg{txO NIOxOpUzPMLiaB?= NFzmNpd2eHKnZ4XsZZR{KFCWRV6gdIFzfGmjbHz5JIJ6KGmwaHnibZRqdmdiU4CxMEBidmRiYXP0bZZifGW|IGDUSW4h[W6mIHnuZYN1cX[jdHXzJGFMXA>? MXeyOVc4ODR{Mx?=
SACC-83 NYXIUFViTnWwY4Tpc44hSXO|YYm= MkTyNlAwPDBxOECg{txO MWqyOOKhcA>? NGTJVFF2eHKnZ4XsZZR{KFCWRV6gdIFzfGmjbHz5JIJ6KGmwaHnibZRqdmdiU4CxMEBidmRiYXP0bZZifGW|IGDUSW4h[W6mIHnuZYN1cX[jdHXzJGFMXA>? MkfNNlU4PzB2MkO=
HLCZ01 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2w5qCUPjEEoNM1US=> NU\PSWtJPDhiaB?= MVnEUXNQ MUPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M4LPNVI2PzJ2OEm5
HLCZ01 NIO3Vm1HfW6ldHnvckBCe3OjeR?= MnnUOFDDqM7:TR?= NYjwfFFCOjRiaB?= NIH6bVhFVVOR NUXUd2ZncW6lcnXhd4V{KGGlY4XteYxifGmxbjDv[kBIOC:JMT3wbIF{\SClZXzsd{Bkd22kaX7l[EB4cXSqIFnGUk3PuQ>? MUKyOVczPDh7OR?=
HLCZ01 MlXmRZBweHSxc3nzJGF{e2G7 MmnHOFDDqM7:TR?= NGrJO48zPCCq Mnu4SG1UVw>? Ml61[Y5p[W6lZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiSV\OMe6y M4OyS|I2PzJ2OEm5
HLCZ01 NUXGdXZSTnWwY4Tpc44hSXO|YYm= MlnXOFDDqM7:TR?= NIXVRYczPCCq MmDzSG1UVw>? M2CwPIlv[3KnYYPld{BVWkGLTDDlfJBz\XO|aX;uJINwdWKrbnXkJJdqfGhiSX70[ZJn\XKxbj5OtS=> MojiNlU4OjR6OUm=
MGC803 NUX0NHU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVSwMVYxKM7:TR?= MVS3NkBp NVXVRZNyUUN3ME20O{4zPeLCidMx5qCKPi52MzFOwG0> M2XvelI2PzBzM{e4
SGC7901 NUHqeItvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfISI1MOC14MDFOwG0> M364[lczKGh? NILDXYtKSzVyPUSzMlU{6oDLwsJihKk2NjF{IN88US=> Ml7WNlU4ODF|N{i=
MGC803 NWD1OlFLTnWwY4Tpc44hSXO|YYm= MYm0NOKh|ryP MYS4M|E3NzJ2IHi= NXn5PY5kfXC{ZXf1cIF1eyCFYnytZkBmgHC{ZYPzbY9v M1i4UVI2PzBzM{e4
SGC7901 M1;KdmZ2dmO2aX;uJGF{e2G7 MX:0NOKh|ryP MYC4M|E3NzJ2IHi= M{jVNZVxemWpdXzheJMhS2KuLXKg[ZhxemW|c3nvci=> MVOyOVcxOTN5OB?=
MCF-7  M{jscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxM|ExKM7:TR?= NVvXWoVQPzJiaB?= MYPEUXNQ MnrD[Y5p[W6lZYOgZ4Ft[2m2cnnvcE1qdmS3Y3XkJINmdGxiZ4Lve5RpKGmwaHnibZRqd25? NX;qe|c6OjV4Nke1NVA>
MDA-MB-231  MmrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKxM|ExKM7:TR?= MXK3NkBp MYPEUXNQ MV;lcohidmOnczDjZYxkcXS{aX;sMYlv\HWlZXSgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdg>? NXPST3BmOjV4Nke1NVA>
MDA-MB-231 NF6xV3NHfW6ldHnvckBCe3OjeR?= MXywMVQxKML3TR?= NXTlZWJkPC1{NDDo NETyRZJqdmO{ZXHz[ZMhS0:[LUKgdJJwfGWrbjDlfJBz\XO|aX;uJIlvKGKxdHigeIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NXSzeWpZOjV3OEezNlk>
MCF-7 M1vEPWZ2dmO2aX;uJGF{e2G7 Mnj3NE01OCEEtV2= NV\tfXRWPC1{NDDo NXLvcG1w\W6qYX7j[ZMhfGinIHXm[oVkfHNib3[gWHBCKG:wIFHCR2czKGW6cILld5Nqd28EoB?= NF7VVmUzPTV6N{OyPS=>
MCF7-MX  NFT3Z3RHfW6ldHnvckBCe3OjeR?= NFPScpExNTRyINM1US=> NGixToo1NTJ2IHi= NEnsT4dmdmijbnPld{B1cGViZX\m[YN1eyCxZjDUVGEhd25iQVLDS|Ih\XiycnXzd4lwdsLi MWeyOVU5PzN{OR?=
MDA-MB-231 M3G5Z2Z2dmO2aX;uJGF{e2G7 MWmwMVQxKML3TR?= NYi5U3R2PC1{NDDo NFr1Tnd{fGmvdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEGEQ1eyJJVxKHSxIESuNlchfGmvZYOgeI8h[2:wdILvcEBt\X[nbDDifUAyOiCqwrC= M2HqVFI2PTh5M{K5
A2780 MnnOSpVv[3Srb36gRZN{[Xl? Mn\iOU8yOC9zNTFOwG0> NIXj[lQ1QCCq NUTXPI9z\GWlcnXhd4V{KEOxeD2yJIV5eHKnc4Ppc44hcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUXDS3ExOjV2MkS4PVg>
SKOV3  NGfzPYVHfW6ldHnvckBCe3OjeR?= MXO1M|ExNzF3IN88US=> M1nWclQ5KGh? Ml\s[IVkemWjc3XzJGNwgC1{IHX4dJJme3Orb36gbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MkT2NlU1OjR6OUi=
A2780 NG\DR5dHfW6ldHnvckBCe3OjeR?= M4HOW|UwOTBxMUWg{txO MknQOFghcA>? NH3rPWRmdGW4YYTld{B1cGViZYjwdoV{e2mxbjDv[kBGNWOjZHjldolvKGGwZDDr[ZJifGmw Mkf3NlU1OjR6OUi=
SKOV3  NXn6SplSTnWwY4Tpc44hSXO|YYm= NX7xOVRVPS9zMD:xOUDPxE1? MV[0PEBp NFfmfHRmdGW4YYTld{B1cGViZYjwdoV{e2mxbjDv[kBGNWOjZHjldolvKGGwZDDr[ZJifGmw M3zLeVI2PDJ2OEm4
A2780 M1;SfGZ2dmO2aX;uJGF{e2G7 MWi1M|ExNzF3IN88US=> NFX4V3o1QCCq NHXGOpRl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhVi2lYXTo[ZJqdiCjbnSgWolu\W62aX6= M1y5fFI2PDJ2OEm4
SKOV3  NIfiNYtHfW6ldHnvckBCe3OjeR?= MWm1M|ExNzF3IN88US=> MmrhOFghcA>? NXr6cno5\GWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJI9nKE5vY3HkbIVzcW5iYX7kJHZqdWWwdHnu MnnONlU1OjR6OUi=
A2780 NUDidVVbTnWwY4Tpc44hSXO|YYm= M2HN[VUwOTBxMUWg{txO MYqxJIg> NIGwR3RqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YheC2DS2SgZY5lKHBvRWLLJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4nkeFI2PDJ2OEm4
SKOV3  MVjGeY5kfGmxbjDBd5NigQ>? MmnROU8yOC9zNTFOwG0> NUjjbG0{OSCq MnrXbY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJJAuSUuWIHHu[EBxNUWUSzDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NWW2cG97OjV2MkS4PVg>
HCT-15 MUPGeY5kfGmxbjDBd5NigQ>? NUWyeVIyOTBvNUCg{txO M1L0OVYuOzZiaB?= NWTyfWlMcW6mdXPld{B1cGViZYjwdoV{e2mxbjDv[kBEV1hvMjDpckBjd3SqIHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> NVTvUIQyOjV{MUiwNlg>
HT-29  NYeydY5LTnWwY4Tpc44hSXO|YYm= NWPxSFY6OTBvNUCg{txO NGfZWIw3NTN4IHi= NELIeYNqdmS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mJGNQYC1{IHnuJIJwfGhiZH;z[UBidmRidHnt[UBl\XCnbnTlcpQhdWGwbnXy NY\nXmZCOjV{MUiwNlg>
HSC3  MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWPQUI5jOOLCk{SwJO69VQ>? NInaW5c1QCCq NVjWbGFRUUN3ME2yOU42yrFzLke4NEDPxE1? NE\IPGozPTF7OEe4PS=>
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HSC3  NWPGXIFXTnWwY4Tpc44hSXO|YYm= NIDIfmkzPSEQvF2= NXPIRlNNPDhiaB?= MVflfIhq[mm2czDzbYdvcW[rY3HueIx6KHKnZIXj[YQhdWmpcnH0bY9vKGOxbXLpcoVlKHerdHigR2VV NEPzR3AzPTF7OEe4PS=>
HSC3  MnK0SpVv[3Srb36gRZN{[Xl? M3nY[lI2KM7:TR?= NULNfIhXPDhiaB?= M1\EbYlvcGmkaYTzJGhUSzNiY3XscEBqdn[jc3nvckBkd22kaX7l[EB4cXSqIFPFWC=> NFfwTIEzPTF7OEe4PS=>
HSC3  M4jMPWZ2dmO2aX;uJGF{e2G7 MYOyOUDPxE1? MXy3NkBp M1y3XIRm[3KnYYPld{BOVVBvMjDhcoQhVU2SLUmgdJJwfGWrboRCpC=> Mn7nNlUyQTh5OEm=
201T  MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3tbY5mPzJiaB?= MUTEUXNQ MmDETWM2OD12OD62JOK2VQ>? NHHsNGQzPTB3N{m0NS=>
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Hep-2 MXzBdI9xfG:|aYOgRZN{[Xl? NE\XcHo2OCEQvF2= M2ThZVAuPDhiaB?= MXrEUXNQ NHj6UXRqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUh\GWyZX7k[Y51KG2jbn7ldi=> NUXpTYNIOjR7OUi1OlQ>
Hep-2 MnntSpVv[3Srb36gRZN{[Xl? Mo\yOVAh|ryP NWGwPW5mOC12ODDo NEm1O3JFVVOR MXvy[YR2[2W|IITo[UB1\WyxbXXyZZNmKGGldHn2bZR6KGe{YXT1ZYxtgQ>? MnzFNlQ6QTh3NkS=
Hep-2 MUXGeY5kfGmxbjDBd5NigQ>? MY[1NEDPxE1? M2rXXlAuPDhiaB?= MnTuSG1UVw>? NFXESVBl\WO{ZXHz[ZMhfGinIH3SUmEh\XiycnXzd4lwdiCxZjDoWGVTXA>? NVPkVWZ1OjR7OUi1OlQ>
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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 2年-20℃
6月-80℃in solvent
別名 SC 58635
溶解度 (25°C) * In vitro DMSO 76 mg/mL (199.28 mM)
エタノール 33 mg/mL (86.53 mM)
<1 mg/mL (<1 mM)
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

カスタマーフィードバック (2)


Click to enlarge
Rating
Source Br J Pharmacol, 2014, 171(2), 498-508. Celecoxib purchased from Selleck
Method Metabolic evaluation
Cell Lines Wild-type and EC-AMPK mice
Concentrations 50 mg·kg−1 ·day−1
Incubation Time 4 weeks
Results The treatment with either drughad no effects on body weight and blood glucose levels(A), but significantly decreased the circulating triglyceride and cholesterol levels in EC-AMPK mice (B).

Click to enlarge
Rating
Source J Cell Physiol, 2014, 10.1002/jcp.24843. Celecoxib purchased from Selleck
Method Live-dead assay
Cell Lines HCC38 cells
Concentrations 5.0 uM
Incubation Time 24 h
Results Initial studies examined whether there was a toxic interaction between the PDE5 inhibitor sildenafil and the non-steroidal anti-inflammatory drug celecoxib. In mammary carcinoma cell lines growing in 10% fetal calf serum sildenafil and celecoxib interacted in a greater than additive fashion to kill parental wild type tumor cells as well as anoikis resistant variants of these cells.

文献中の引用 (6)

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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