Posaconazole (SCH 56592)

Catalog No.S1257

For research use only.

Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.

Posaconazole (SCH 56592) Chemical Structure

CAS No. 171228-49-2

Selleck's Posaconazole (SCH 56592) has been cited by 21 publications

Purity & Quality Control

Choose Selective P450 (e.g. CYP17) Inhibitors

Other P450 (e.g. CYP17) Products

Biological Activity

Description Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.
Features Currently the most advanced candidate for the treatment of Chagas disease.
Targets
lanosterol 14α-demethylase [1] CYP3A4 [6]
In vitro

Posaconazole has potent trypanocidal activity. Amiodarone acts synergistically with Posaconazole. Posaconazole also affects and disrupts Ca2+ homeostasis in T. cruzi. Posaconazole blocks the biosynthesis of ergosterol, which is essential for parasite survival. Posaconazole has a clear, dose-dependent effect on proliferation of the epimastigote (extracellular) stages, with a minimal inhibitory concentration of 20 nM and an IC50 of 14 nM. Against the clinically relevant intracellular amastigote form of the parasite, Posaconazole is even more potent. Posaconazole has the minimal inhibitory concentration and IC50 values of 3 nM and 0.25 nM. [1] Posaconazole is active against isolates of Candida and Aspergillus spp. that exhibit resistance to Fluconazole, Voriconazole, and Amphotericin B and is much more active than the other triazoles against zygomycetes. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human hepatocytes NFPNWVZHfW6ldHnvckBie3OjeR?= MUPJcohq[mm2aX;uJI9nKEO\UEPBOEBqdiCqdX3hckBp\XCjdH;jfZRmeyC3c3nu[{B1\XO2b4P0[ZJwdmViYYOgd5Vje3S{YYTlJIJ6KEiSTFOvUXMwVVNibXX0bI9lNCCLQ{WwQVAvODVizszN MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl2OEW2OUc,OjR7NEi1OlU9N2F-
3T3 NWXzWFN5SW62aYTyfZBidm:|b33hcEBie3OjeR?= NULafZlQSW62aYTyfZBidm:|b33hcEBi[3Srdnn0fUBi\2GrboP0JHRzgXCjbn;zc41iKGO{dYrpJHR2dGGqdXXuJIlv\mWldHXkJIlvKG2xdYPlJFNVOyClZXzsd{whTUN3ME2wMlAxODQQvF2= M4jKS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEe1NlgzLz5zOUi3OVI5OjxxYU6=
BESM M{jsV2Z2dmO2aX;uJIF{e2G7 NGryfHI2KHWP NWnEblM2PzJiaILz NGPsSlRKdmirYnn0bY9vKG:oIIP0[ZJwdCBzND3hcJBp[S2mZX3leIh6dGG|ZTDpckBVenmyYX7vd49u[SClcoX6bUBmeGmvYYP0bYdwfGW|IHnu[oVkfGWmIHnuJGJGW01iY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJI9nKGyjbn;zeIVzd2xiYX7kJIVjfXKrY3;sJJBz\WO3coPvdpMh[XRiNTD1UUBi\nSncjC3NkBpenN? M{TyU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{i1PFc2Lz5{MEO4OVg4PTxxYU6=
BESM NGrBUoFHfW6ldHnvckBie3OjeR?= MnzwOUB2VQ>? MWK3NkBpenN? M2S1dGlvcGmkaYTpc44hd2Zic4Tldo9tKDF2LXHsdIhiNWSnbXX0bJlt[XOnIHnuJHRzgXCjbn;zc41iKGO{dYrpJIVxcW2jc4Tp[491\XNiaX7m[YN1\WRiaX6gRmVUVSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6g[ZBqe3Sncn;sJINwdnSnboSgZZQhPSC3TTDh[pRmeiB5MjDodpM> Mn22QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|OEW4O|UoRjJyM{i1PFc2RC:jPh?=
BESM NITUOmJHfW6ldHnvckBie3OjeR?= NVjIOIJpPSC3TR?= M3vMOFczKGi{cx?= NVT6bJNiUW6qaXLpeIlwdiCxZjDzeIVzd2xiMUStZYxxcGFvZHXt[ZRpgWyjc3WgbY4hXHK7cHHuc5NwdWFiY4L1fokh\XCrbXHzeIlod3SnczDpcoZm[3SnZDDpckBDTVOPIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBn\WOxc4Tldo9tKGOxboTlcpQh[XRiNTD1UUBi\nSncjC3NkBpenN? NHH1eW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO4OVg4PSd-MkCzPFU5PzV:L3G+
BESM MWXGeY5kfGmxbjDhd5NigQ>? NWLaTpZDPSC3TR?= NHPVfpI4OiCqcoO= MXzJcohq[mm2aX;uJI9nKHO2ZYLvcEAyPC2jbIDoZU1l\W2ndHj5cIF{\SCrbjDUdplx[W6xc3;tZUBkenW8aTDhcYF{fGmpb4Tld{Bqdm[nY4Tl[EBqdiCERWPNJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCxZjDsZY5we3Sncn;sJIFv\CCnYoXybYNwdCCycnXjeZJ{d3K|IHH0JFUhfU1iYX\0[ZIhPzJiaILz NYXvXlRKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzPFU5PzVpPkKwN|g2QDd3PD;hQi=>
BESM M{m2cmZ2dmO2aX;uJIF{e2G7 NH\DZ2Q2KHWP NUXyb4tZPzJiaILz NWTWWFExUW6qaXLpeIlwdiCxZjDzeIVzd2xiMUStZYxxcGFvZHXt[ZRpgWyjc3WgbY4hXHK7cHHuc5NwdWFiY4L1fokh[W2jc4Tp[491\XNiaX7m[YN1\WRiaX6gRmVUVSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6g[ZBqe3Sncn;sJINwdnSnboSgZZQhPSC3TTDh[pRmeiB5MjDodpM> NH;NWVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO4OVg4PSd-MkCzPFU5PzV:L3G+
BESM M4PVemZ2dmO2aX;uJIF{e2G7 MXy1JJVO NIDuXHM4OiCqcoO= MoqyTY5pcWKrdHnvckBw\iC|dHXyc4whOTRvYXzwbIEu\GWvZYTofYxie2ViaX6gWJJ6eGGwb4PvcYEh[3K3enmgZY1ie3SrZ3;0[ZMhcW6oZXP0[YQhcW5iQlXTUUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iZnXjc5N1\XKxbDDjc451\W62IHH0JFUhfU1iYX\0[ZIhPzJiaILz MmHMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|OEW4O|UoRjJyM{i1PFc2RC:jPh?=
SJ-GBM2 Ml;YdWhVWyCjc4PhfS=> NH7nUIlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODR{OUWxNUc,OjB2Mkm1NVE9N2F-
NB-EBc1 M1y0N5FJXFNiYYPzZZk> NF7LVXpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NILaWYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW0O|gyQSd-MkC1OFc5OTl:L3G+
SK-N-SH MnT0dWhVWyCjc4PhfS=> NIHST|RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> MkjTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3NEe4NVkoRjJyNUS3PFE6RC:jPh?=
OHS-50 Mo[wdWhVWyCjc4PhfS=> NUjNS2pYeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NHvWdFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW0O|gyQSd-MkC1OFc5OTl:L3G+
A673 MmOzdWhVWyCjc4PhfS=> NVjP[4J1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= NE\nZXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2NlcyOyd-MkO0OlI4OTN:L3G+
SK-N-MC M2LpTpFJXFNiYYPzZZk> MkDRdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= M1LvdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUKwOVM6Lz5{NEGyNFU{QTxxYU6=
BT-37 NF\NeHNyUFSVIHHzd4F6 MWLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? Mkj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|MESxOVAoRjJ2M{C0NVUxRC:jPh?=
C2C12 MlnHSpVv[3Srb36gZZN{[Xl? NH;hZmEyODBibl2= M{m1dlI1KGi{cx?= MUjJcohq[mm2aX;uJI9nKHO2ZYLvcEBjcW:|eX70bIV{cXNiaX6gWJJ6eGGwb4PvcYEh[3K3enmgR2FKNzd{IHHtZZN1cWexdHXzJIlv\mWldHXkJIlvKG2xdYPlJGMzSzF{IHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJIxidm:|dHXyc4whdGW4ZXygZZQhOTByIH7NJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IFfDMW1UKG2ndHjv[C=> NYjtSnFZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzPVM3PDZpPkK1N|k{PjR4PD;hQi=>
C2C12 MXHGeY5kfGmxbjDhd5NigQ>? M1\KZlExOCCwTR?= NI\SWlIzPCCqcoO= MVTJcohq[mm2aX;uJI9nKHO2ZYLvcEBjcW:|eX70bIV{cXNiaX6gWJJ6eGGwb4PvcYEh[3K3enmgR2FKNzd{IHHtZZN1cWexdHXzJIlv\mWldHXkJIlvKG2xdYPlJGMzSzF{IHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJIVjfXKrY3;sJIxmfmWuIHH0JFExOCCwTTDpcoN2[mG2ZXSg[o9zKDJ2IHjyd{BjgSCJQz3NV{Bu\XSqb3S= NH6yTmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO5N|Y1Pid-MkWzPVM3PDZ:L3G+
C2C12 NFT5S|JHfW6ldHnvckBie3OjeR?= NHLlUpYyODBibl2= NUi5PYwxOjRiaILz NXO3OGk4UW6qaXLpeIlwdiCxZjDzeIVzd2xiYnnvd5lvfGinc3nzJIlvKFS{eYDhco9{d22jIHPyeZpqKEODST:3NkBidWG|dHnnc5RmeyCrbn\lZ5Rm\CCrbjDtc5V{\SCFMlOxNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iZYDpd5Rmem:uIHzleoVtKGG2IEGwNEBvVSCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBISy2PUzDt[ZRpd2R? MkjPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUO2OFYoRjJ3M{mzOlQ3RC:jPh?=
C2C12 MlPsSpVv[3Srb36gZZN{[Xl? NXS5NY5ZOTByIH7N MW[yOEBpenN? M3HGVGlvcGmkaYTpc44hd2Zic4Tldo9tKGKrb4P5cpRp\XOrczDpckBVenmyYX7vd49u[SClcoX6bUBESUlxN{KgZY1ie3SrZ3;0[ZMhcW6oZXP0[YQhcW5ibX;1d4UhSzKFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKG[nY3;zeIVzd2xibHX2[Ywh[XRiMUCwJI5OKGmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JGdENU2VIH3leIhw\A>? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN7M{[0Okc,OjV|OUO2OFY9N2F-
LAN-5 NFT3V4tyUFSVIHHzd4F6 M3XSVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzBzNEmyNkc,OjdyMUS5NlI9N2F-
ASZ NV3SNHlwTnWwY4Tpc44h[XO|YYm= MnzOOFghcHK| NWDoPXpRUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDwZZRpf2G7IHnuJI1wfXOnIFHTXkBk\WyuczDhd5Nme3OnZDDhd{Bld3ewcnXneYxifGmxbjDv[kBIdGlzIH3SUmEh\XiycnXzd4lwdiCjZoTldkA1QCCqcoOgZpkheVCFUjDt[ZRpd2RuIFnDOVA:OC53NN88US=> NV;kV3dURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNVQ6OjJpPkK3NFE1QTJ{PD;hQi=>
MERP MB M2jpZ2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYP5[4lsPDhiaILz NGDleYpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIF3FVnAhVUJiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckB2e2mwZzDt[ZRpgWxvW{PIYZRpgW2rZHnu[UBi\nSncjC0PEBpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44he3CnY4Tyc5Bpd3SxbXX0dpktKEeLNUC9NU42|ryP M4XT[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEG0PVIzLz5{N{CxOFkzOjxxYU6=
J774 M{\TNGFvfGmuZXnzbI1idmmjbDDhd5NigQ>? MXq3NkBpenN? MlP1RY51cWynaYPocYFvcWGuIHHjeIl3cXS7IHHnZYlve3RiTHXpd4hu[W6rYTDhcYF7d26nboPpd{Bqdm[nY4Tl[EBqdiCvb4Xz[UBLPzd2IHPlcIx{KGGodHXyJFczKGi{czD1d4lv\yB{IHjyd{Bx[XKjc3n0[UBmgHCxc3XkJI1wfXOnIFq3O|Qh[2WubIOsJGlEPTB;MT62{txO NWHQR4pYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewOFg6PDNpPkK3NFQ5QTR|PD;hQi=>
ASZ MofKSpVv[3Srb36gZZN{[Xl? MYe0PEBpenN? NFe2doJKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIFHTXkBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCJbHmxJI1TVkFiZYjwdoV{e2mxbjDh[pRmeiB2ODDodpMh[nlicWLUMXBEWiCjbnHsfZNqeyxiSVO1NF0xNjYQvF2= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODV{OU[zOUc,OzB3Mkm2N|U9N2F-
Ptch-CKO NGi4SIRHfW6ldHnvckBie3OjeR?= MW\Jcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIHjl[IdmcG:pLXTldIVv\GWwdDDtc5V{\SCSdHPoMWNMVyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpNCCJSUWwQVEvPc7:TR?= NEHsbYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVY{PSd-M{C1Nlk3OzV:L3G+
Caco2 NUTWWFdyTnWwY4Tpc44h[XO|YYm= NF[1WJRUfWK|dILheIUh[WO2aY\peJkh[XRiUD3ndEBqdiCqdX3hckBE[WOxMjDj[YxteyCkeTDMR{1OWy:PUzDhcoFtgXOrcx?= NWjnTJNoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1Nlk3OzVpPkOwOVI6PjN3PD;hQi=>
Vero MmfSRY51cX[rcnHsJIF{e2G7 MkL6RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgSGVPXjJiMU[4PFEhcW6oZXP0[YQhcW5iQX\ybYNidiCpcnXlckBud26tZYmgWoVzdyClZXzsd{BjgSCzUmStVGNTKGGwYXz5d4l{NCCHQ{WwQVQvOc7:TR?= Ml\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzFzMki0OFcoRjNzMUK4OFQ4RC:jPh?=
Caco-2 NFviW4dHfW6ldHnvckBie3OjeR?= NVnjfJVqPDhiaILz NW\SfWNOTGW2ZYLtbY5ifGmxbjDv[kBKSzVyII\hcJVmeyCob4KgbY5pcWKrdHnvckBw\iCVQWLTMWNwXi1{IHnu[JVk\WRiY4n0c5RwgGmlaYT5JI9nKEOjY3:tNkBk\WyuczDh[pRmeiB2ODDoc5VzeyCkeTDobYdpKGOxboTlcpQhcW2jZ3nu[{whUUN3ME2xMlYy|ryP NFXTUmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOzl5Lze+R4hGVUKOPD;hQi=>
Caco-2 M{L6VmZ2dmO2aX;uJIF{e2G7 M3LSd|Q5KGi{cx?= NWfhTlVbXG:6aXPpeJkh[WejaX7zeEBE[WOxLUKgZ4VtdHNiZHX0[ZJucW6nZDDheEA1QCCqb4Xyd{BjgSCrboTyZYNmdGy3bHHyJGFVWCClb37j[Y51emG2aX;uJJV{cW6pIITo[UBE\WyuVHn0[ZIuT2yxIFz1cYlv\XOlZX70JGNmdGxiVnnhZoltcXS7IFHzd4F6NCCFQ{WwQVE1NjZ2zszN NGjWOYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOzl5Lze+R4hGVUKOPD;hQi=>
Assay
Methods Test Index PMID
Growth inhibition assay Cell proliferation 28383032
Western blot Wee1 / c-Myc / Cyclin B1 / Cdc25C / Bcl-2 / Bax / p21 / Survivin 28383032
In vivo Treatment of infected animals with amiodarone alone reduces parasitemia, increases survival 60 days pi (0% for untreated controls vs 40% for amiodarone-treated animals) and, when given in combination with Posaconazole, delays the development of parasitemia. [1] Coadministration of Posaconazole and Boost Plus increases drug exposure compared to the administration of Posaconazole alone in the fasted state. Food, particularly meals high in fat content, significantly increases Posaconazole bioavailability. Systemic exposure to Posaconazole increases 4- and 2.6-fold when it is consumed with a high-fat and nonfat meal, respectively. [3] Posaconazole and Amiodarone may constitute an effective anti-T. cruzi therapy with low side effect. [4] At twice-daily doses of ≥15 mg/kg of body weight, Posaconazole prolongs the survival of the mice and reduces tissue burden. [5]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: Epimastigote form of T. cruzi amastigotes
  • Concentrations: 0 nM -4 nM
  • Incubation Time: 96 hours
  • Method:

    The epimastigote form of the parasite is cultivated in liver infusion tryptose medium, supplemented with 10% new born calf serum at 28 °C with strong (120 rpm) agitation. Cultures are initiated at a cell density of 2 × 106 epimastigotes/mL, and Posaconazole is added at a cell density of 0.5−1.0 × 107 epimastigotes/mL. Cell densities are measured by using an electronic particle counter as well as by direct counting with a hemocytometer. Cell viability is followed by Trypan blue exclusion, using light microscopy. Amastigotes are cultured in Vero cells maintained in minimal essential medium supplemented with 1% fetal calf serum in a humidified atmosphere (95% air−5% CO2) at 37 °C. Cells are infected with 10 tissue culture-derived trypomastigotes per cell for 2 hours and then washed three times with phosphate-buffered saline (PBS) to remove nonadherent parasites. Fresh medium with and without Posaconazole is added, and the cells are incubated for 96 hours with a medium change at 48 hours. The percent of infected cells and the numbers of parasites per cell are determined directly using light microscopy, and a statistical analysis of the results is carried out. IC50 values are calculated by nonlinear regression, using the program GraFit. Fractional inhibitory concentrations (FIC) are calculated. Cytoplasmic free Ca2+ concentrations in control and drug-treated extracellular epimastigotes are determined by fluorimetric methods using Fura-2. Subcellular Ca2+ levels and mitochondrial membrane potentials are monitored on individual Vero cells infected with T. cruzi amastigotes by using time-scan confocal microscopy. Briefly, Vero cells heavily infected (72 hours) with T. cruzi amastigotes are plated onto 22 × 40 mm glass coverslips (0.15 mm thickness) and incubated simultaneously with 10 μM cell-permeant Rhod-2 and 10 μg/mL Rhodamine-123 for 50 minutes at 37 °C in culture medium and then washed and incubated with Ringer's solution, with or without amiodarone. Under the conditions used fluorescence of Rhod-2 comes mainly from intracellular Ca2+-rich compartments, like mitochondria, since its low affinity for Ca2+ limits its fluorescence in the Ca2+-poor cytoplasm of the Vero cells or amastigotes. Rhodamine-123 is a mitochondrion-specific cationic dye, which distributes across the inner mitochondrial membranes strictly according to their membrane potential.

Animal Research:

[1]

  • Animal Models: Female NMRI−IVIC mice with acute Chagas
  • Dosages: 20 mg/kg/d
  • Administration: Oral

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 700.78
Formula

C37H42F2N8O4

CAS No. 171228-49-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(C(C)O)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OCC5CC(OC5)(CN6C=NC=N6)C7=C(C=C(C=C7)F)F

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
NCT04825275 Not yet recruiting Drug: Posaconazole Pill Glioblastoma|Glioblastoma Multiforme|Glioblastoma Multiforme of Brain|Glioblastoma Multiforme Adult Milton S. Hershey Medical Center January 2022 Early Phase 1
NCT04771130 Recruiting Drug: BGB-11417|Drug: Azacitidine|Drug: Posaconazole Acute Myeloid Leukemia|Myelodysplastic Syndromes|Myelodysplastic/Myeloproliferative Neoplasm BeiGene May 24 2021 Phase 1|Phase 2
NCT04725942 Not yet recruiting Drug: Oral Posaconazole tablets Pulmonary Fungal Infection Institute of Hematology & Blood Diseases Hospital|Shanxi Bethune Hospital|The Second Hospital of Hebei Medical University|Tianjin Medical University Cancer Institute and Hospital January 2021 --
NCT03717623 Recruiting Drug: Posaconazole pharmacokinetics Posaconazole|Pharmacokinetics|Invasive Candidiases|Invasive Aspergillosis|Invasive Mycosis|Fungal Infection|Prophylaxis Melbourne Health|Merck Sharp & Dohme Corp. August 1 2019 Phase 4

(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 Posaconazole (SCH 56592) | Posaconazole (SCH 56592) supplier | purchase Posaconazole (SCH 56592) | Posaconazole (SCH 56592) cost | Posaconazole (SCH 56592) manufacturer | order Posaconazole (SCH 56592) | Posaconazole (SCH 56592) distributor