Home Proteases HIV Protease inhibitor - COVID-19 inhibitor Nelfinavir (AG 1343) Mesylate

Nelfinavir (AG 1343) Mesylate

Catalog No.S4282 Synonyms: Viracept

For research use only.

Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.

Nelfinavir (AG 1343) Mesylate Chemical Structure

CAS No. 159989-65-8

Selleck's Nelfinavir (AG 1343) Mesylate has been cited by 15 publications

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Biological Activity

Description Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.
Targets
HIV protease [1]
(Cell-free assay)
2 nM(Ki)
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa Mk\USpVv[3Srb36gZZN{[Xl? NGL0WYRVWF:WUlHOV3BQWlSHUkqgbY5pcWKrdHnvckBw\iCWRVGgeZB1[WunIDjUSWE7KDFyIIXNLUBqdiCRQ2SxMYV5eHKnc4PpcochUGWOYTDj[YxteyxiSVO1NF0zOS56zszNMi=> NV7ZXWxzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUC2PFE{PzhpPkGwOlgyOzd6PD;hQi=>
Caco-2 NHPLblNHfW6ldHnvckBie3OjeR?= NEXGdWlVWF:WUlHOV3BQWlSHUkqgbY5pcWKrdHnvckBw\iCGYYXuc5J2[mmlaX6geJJidnOncHn0bIVtcWGuIITyZY5{eG:{dDCoZoF{[WxidH:gZZBq[2GuKTCoSIF2dm:{dXLpZ4lvQiB3IIXNLUBqdiCFYXPvMVIh[2WubIOsJGlEPTB;MT60{txONg>? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODh{MEGzO{c,OTB6MkCxN|c9N2F-
MT-4 MWfBcpRqfmm{YXygZZN{[Xl? M4DsemFvfGlvSFnWMVEh[WO2aY\peJkh[WejaX7zeEBYcWymIIT5dIUhfmm{dYOgbY4hVVRvNDDj[YxteyxiRVS1NF0xNjB{zszNMi=> NI\oTVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUW0N|Y4Pyd-MUG1OFM3Pzd:L3G+
MT-4 NHnVUFNCdnSrdnnyZYwh[XO|YYm= NVz5[WRxSW62aT3ITXYuOSCjY4Tpeol1gSCjZ3HpcpN1KG23dHHueEBJUVZvMTDpckBOXC12IHPlcIx{KCivdYTheIlwdiC|ZXzlZ5Rm\CC5aYToJINwdXCxdX7kJFEqNCCHREWwQVAvODgQvF2u Mon2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF3NEO2O|coRjFzNUSzOlc4RC:jPh?=
MT-4 M4LCZWFvfGm4aYLhcEBie3OjeR?= Ml3BRY51cS2KSW[tNUBi[3Srdnn0fUBi\2GrboP0JI12fGGwdDDITXYuOSCrbjDNWE01KGOnbHzzJEhufXSjdHnvckB{\WynY4Tl[EB4cXSqIILpeI9v[X[rcjmsJGVFPTB;MD6xNe69VS5? NG\rcmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUW0N|Y4Pyd-MUG1OFM3Pzd:L3G+
MT-4 MUXBcpRqfmm{YXygZZN{[Xl? NEXzNHNCdnSrLVjJWk0yKGGldHn2bZR6KGGpYXnud5QhdXW2YX70JGhKXi1zIHnuJG1VNTRiY3XscJMhMG23dHH0bY9vKHOnbHXjeIVlKHerdHigd4FyfWmwYY\pdkktKEWGNUC9NE4yOs7:TT6= MluzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF3NEO2O|coRjFzNUSzOlc4RC:jPh?=
MT-4 MnTkRY51cX[rcnHsJIF{e2G7 MUPBcpRqNUiLVj2xJIFkfGm4aYT5JIFo[Wmwc4SgcZV1[W62IFjJWk0yKGmwIF3UMVQh[2WubIOgLI12fGG2aX;uJJNmdGWldHXkJJdqfGhibnXs[olv[X[rcjmsJGVFPTB;Mj60OO69VS5? NGHS[GU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUW0N|Y4Pyd-MUG1OFM3Pzd:L3G+
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LLC-PK1 NXLqc3kyTnWwY4Tpc44h[XO|YYm= NED5dXJVWF:WUlHOV3BQWlSHUkqgbY5pcWKrdHnvckBw\iCFYXzj[YlvNUGPIHXm[ox2gCCrbjDN[JIy[S2neIDy[ZN{cW6pIFzMR{1RUzFiY3XscJMtKEmFNUC9Nk4{|ryPLh?= M3q1WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{Nkm5N|g6Lz5zMk[5PVM5QTxxYU6=
LLC-PK1 NUH3[5JVTnWwY4Tpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMEBpfW2jbjDMMW1FWjFiZYjwdoV{e2WmIHnuJGxNSy2SS{Gg[ZBqfGinbHnhcEBk\WyuczD1d4lv\yClYXzj[YlvNUGPIIDvcIFzcXOjdHnvckBie3OjeTygTWM2OD1|LkVOwG0v MmHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJ4OUmzPFkoRjF{Nkm5N|g6RC:jPh?=
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HEK NHW4UGxHfW6ldHnvckBie3OjeR?= NYnpepp5XFChVGLBUnNRV1KWRWK6JIlv[3KnYYPlJIlvKG2rdH;4ZY51em:wZTDpcpRz[WOnbHz1cIFzKGGlY4XteYxifGmxbjDpckBDS1KSLXX4dJJme3OrbnegTGVMKGOnbHzzMEBKSzVyPUGyMlXPxE1w M1P6dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MEC3NVAzLz5zNUCwO|ExOjxxYU6=
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HOG.R5 MUPBcpRqfmm{YXygZZN{[Xl? NXH4XYhQPCCmYYnz MXjBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIFjPS{5TPSClZXzsd{Bi\nSncjC0JIRigXNuIFnDOVA:OC5yOd88UU4> NFWyNHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUKxO|I5OSd-MUWyNVczQDF:L3G+
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PHA-PBMC Ml3xRY51cX[rcnHsJIF{e2G7 NUK0W3R2SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDCRU1NKGm|b3zheIUhcW5iaIXtZY4hWEiDLWDCUWMh[2WubIOsJGlEPTB;MD6wNFfPxE1w MnqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ7MUO3NVQoRjF4OUGzO|E1RC:jPh?=
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PHA-PBMC NGfMZndCdnSrdnnyZYwh[XO|YYm= M{fD[2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JI12dHSrIHTyeYcuemW|aYP0ZY51KEiLVkGgS{B3[XKrYX70JIlvKGi3bXHuJHBJSS2SQl3DJINmdGy|LDDJR|UxRTBwMUhOwG0v NV\VTpZ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[5NVM4OTRpPkG2PVE{PzF2PD;hQi=>
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RD MlzidWhVWyCjc4PhfS=> Ml7jdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ M2fUWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) NHr5[3ZyUFSVIHHzd4F6 MlP4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| NEPHUWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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HepG2 M4P1OWN6fG:2b4jpZ4l1gSCjc4PhfS=> NUnZ[XdKPSCmYYnz NYLle4RRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEWg[IF6eyCkeTDYWHQh[XO|YYmsJGNEPTB;Nz60{txONg>? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1PFQwLz6FaFXNRmw9N2F-
skeletal myoblast cells M4PLfGN6fG:2b4jpZ4l1gSCjc4PhfS=> NGnFT3U4OiCqb4Xydy=> NYiyeIpoTE6GSUqgR5l1d3SxeHnjbZR6KGmwIG\peJJwNCB5MjDoc5VzNCCrbjDyZZQhe2unbHX0ZYwhdXmxYnzhd5Qh[2WubIOsJGlEPTB;MUKuNFXPxE1w MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1PFQwLz6FaFXNRmw9N2F-
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Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 22271897
Western blot p-eIF2Aα / eIF2Aα / ATF4 / GRP78 / CHOP ; SOD1 / SOD2 / catalase ; PAX3 / MITF 21697087 27280849 26977879
Immunofluorescence LC3 / p62 ; PAX3 / MITF ; p-SMAD2 27330277 26977879
In vivo In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. Initial investigation of the compound in fed rats indicated an oral bioavailability of 43%. In contrast, the oral bioavailability was significantly reduced in fasted rats to 29%. Nelfinavir demonstrated significant oral bioavailabilability across a range of species including dogs (47%), marmosets (17%), and cynomolgus monkeys (26%). It has a long plasma half-life after oral dosing that is likely due to a combination of slow dissolution and absorption. nelfinavir is well absorbed in humans particularly when administered with food and possesses minimal and easily managed side effects[1].

Protocol (from reference)

Animal Research:

[1]
  • Animal Models: Sprague-Dawley rats
  • Dosages: 12.5 to 25 mg/kg (i.v); 25 to 50 mg/kg (oral)
  • Administration: i.v and oral administration

Solubility (25°C)

In vitro

 DMSO 100 mg/mL
(150.62 mM)
Water Insoluble
Ethanol ''100 mg/mL

Chemical Information

Molecular Weight 663.89
Formula

C33H49N3O7S2
CAS No. 159989-65-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O.CS(=O)(=O)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

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

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