Daclatasvir (BMS-790052)

For research use only.

Catalog No.S1482 Synonyms: EBP883

46 publications

Daclatasvir (BMS-790052) Chemical Structure

CAS No. 1009119-64-5

Daclatasvir (BMS-790052, EBP883) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

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Selleck's Daclatasvir (BMS-790052) has been cited by 46 publications

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Choose Selective HCV Protease Inhibitors

Biological Activity

Description Daclatasvir (BMS-790052, EBP883) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.
Features First-in-class, highly selective inhibitor of hepatitis C virus (HCV) NS5A with picomolar EC50 values.
Targets
HCV NS5A [1]
9 pM-50 pM(EC50)
In vitro

BMS-790052 is one of the most potent inhibitors of HCV replication reported so far. The mean EC50 valuses of BMS-790052 are 50 and 9 pM for HCV genotype 1a and 1b replicons, respectively. BMS-790052 displays a therapeutic index (CC50/EC50) of at least 105 and is inactive towards a panel of 10 RNA and DNA viruses, with EC50 higher than 10 μM. This confirms BMS-790052's specificity for HCV. [1] In Huh7 cells harboring the HCV genotype 1b replicons, BMS-790052 blocks both transient and stable HCV genome replication, with EC50 values raging from 1-15 pM. BMS-790052 (100 pM or 1 nM) has been shown to alter the subcellular localization and biochemical fractionation of NS5A. [2] BMS-790052 inhibits hybrid replicons containing HCV genotype-4 NS5A genes with EC50 of 7-13 pM. Residue 30 of NS5A is an important site for BMS-790052-mediated resistance in the hybrid replicons. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CEM cells MV7DfZRwfG:6aXPpeJkh[XO|YYm= NUXa[oVuOyCmYYnz Mk[5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR2VOKGOnbHzzJIFnfGW{IEOg[IF6eyxiQ1O1NF06NjZizszN NXHUeoc6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxOVQ4OTRpPkK1NVU1PzF2PD;hQi=>
Huh7 NGf1c2NCdnSrdnnyZYwh[XO|YYm= Mmq5N{Bl[Xm| NWHWOZR7SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHiJIlv\mWldHXkJIlvKGi3bXHuJGh2cDdiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JINmdGxvYnHz[YQhemWybHnjc44h[XO|YYmsJGVEPTB;MD6wNFAxODQQvF2= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF2OEGwNEc,OjVzNEixNFA9N2F-
Huh-luc/neo-ET replicon MULBcpRqfmm{YXygZZN{[Xl? M3y1TFQ5KGi{cx?= MUPBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDI[ZBifGm2aYOgR{B3cXK3czDn[Y5wfHmyZTCxZkBp[XKkb4LpcochVlN3QTDMNlhXKG23dHHueEBo\W6nIHnuJGh2cC2udXOvcoVwNUWWIILldIxq[2:wIHPlcIx{KGGodHXyJFQ5KGi{czDifUB1emGwc3nlcpQhemWybHnjc44hdXW2YX70MYJie2WmIHz1Z4ln\XKjc3WgZZN{[XluIFXDOVA:OC5yMECwNFTPxE1? Mnq3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NkizNVMoRjJ2NU[4N|E{RC:jPh?=
HuH7 NXXWempySW62aY\pdoFtKGG|c3H5 MVPBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5idnnyZYwhWk6DIILldIxq[2G2aX;uMEBGSzVyPUCuNFAxODB2zszN Ml\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOUm1N|IoRjJ4MEm5OVMzRC:jPh?=
HuH7 NH3WRXVCdnSrdnnyZYwh[XO|YYm= MmDFRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wIHL5JHJVNVCFUjDhcoFtgXOrczygSWM2OD1yLkCwNFAxPjcQvF2= NVvlfZd6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1NFc6PjFpPkKyOVA4QTZzPD;hQi=>
HuH-Lcu-Neo NVLHdI82TnWwY4Tpc44h[XO|YYm= M{T4blQ5KGi{cx?= NW\jUJNIUW6qaXLpeIlwdiCxZjDOV|VCKGmwIFjDWkBo\W6xdInw[UAy[iCrbn\lZ5Rm\CCrbjDIeWguVGO3LV7lc{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5idnnyZYwhemWybHnjZZRqd25iaX7jeYJifGWmIH\vdkA1QCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMECwNFA5Oc7:TR?= M1vzWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzN{MkCyO|gzLz5|MkKwNlc5OjxxYU6=
Huh-5.2 Mn\WRY51cX[rcnHsJIF{e2G7 MX20JIRigXN? MoLmRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGMhfmm{dYOg[4Vvd3S7cHWgNYIhcW6oZXP0[YQhcW5iaIXtZY4hUHWqLUWuNkBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCKQ2[gdoVxdGmlb36gVm5CKHKncHzpZ4F1cW:wIHHmeIVzKDRiZHH5d{BjgSCudXPp[oVz[XOnIHHzd4F6NCCHQ{WwQVAvODByMEC5{txO Mn\3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC4NVEoRjJ2OUCwPFEyRC:jPh?=
HuH7 M4HJSWFvfGm4aYLhcEBie3OjeR?= NHn2N4Y{KGSjeYO= NIHHOFFCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJS1ZiZ3Xuc5R6eGViMXKgR49vOSCrbn\lZ5Rm\CCrbjDoeY1idiCKdVi3JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhWk6DIILldIxq[2G2aX;uJIFnfGW{IEOg[IF6eyCkeTDy[Y5qdGyjIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlAxODByOd88US=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN{MEmzN{c,OjR|MkC5N|M9N2F-
HuH7 MXTBcpRqfmm{YXygZZN{[Xl? Mk\OO|IhcHK| Ml;mRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wIHHmeIVzKDd{IHjyd{BjgSCIUlXUJIF{e2G7LDDFR|UxRTBwMECwNFA6|ryP M37KWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUKxNlk6Lz5{NEWyNVI6QTxxYU6=
HuH7 NUL5[lRUSW62aY\pdoFtKGG|c3H5 M2PPW2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEXiCpZX7veJlx\SBzYjDDc44yKGmwZnXjeIVlKGmwIHj1cYFvKEi3SEegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC4aYLhcEBz\XCuaXPheIlwdixiRVO1NF0xNjByMECwPe69VQ>? NWe2Vmd{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wO|c1QTNpPkK2NFc4PDl|PD;hQi=>
Huh7.5/J6/JFH1/EMCVIRES/hRlucNeo NGKwT2dHfW6ldHnvckBie3OjeR?= NHHzSoc4OiCqcoO= MlXpTY5pcWKrdHnvckBw\iCQU{XBJIlvKEiFVjDn[Y5wfHmyZTCyZUBqdm[nY4Tl[EBqdiCqdX3hckBJfWh5LkWvTlYwUk[KMT;FUWNXUVKHUz;oVox2[06nbzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHKncHzpZ49vKGyndnXsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NE4xODByMEpOwG0> NF7MXnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUexNFQ4QSd-M{G3NVA1Pzl:L3G+
HuH7 replicon NE\mXGtHfW6ldHnvckBie3OjeR?= MmXpNkBl[Xm| NWXLdpd1UW6qaXLpeIlwdiCxZjDOV|VCKGmwIFjDWkBo\W6xdInw[UAy[iCrbn\lZ5Rm\CCrbjDoeY1idiCKdVi3JJJmeGyrY3;uJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC|dXLn[Y5wdWmlII\pdoFtKFKQQTDy[ZBtcWOjdHnvckB1emWjdHXkJIZweiB{IHThfZMh\m:ubH;3[YQh[nliY3;tdI92dmRid3HzbI92fCCjbnSgd5Vje2WzdXXueEBkd22yb4Xu[EBld3OrbnegcYVie3W{ZXSgZYZ1\XJiMTDkZZkh[nliU1XBVEBz\XCxcoTldkBo\W6nLDDFR|UxRTBwMECwNFA6|ryP NH:2PIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEe3NlYxPyd-M{C3O|I3ODd:L3G+
HuH7 M3PKbmFvfGm4aYLhcEBie3OjeR?= NGG5UpBCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJS1ZiMXKgbY5n\WO2ZXSgbY4hcHWvYX6gTJVJPyClZXzsd{BjgSCrbjD2bZRzdyC{ZYDsbYNwdiCjc4PhfUwhTUN3ME2wMlAxODBzzszN NVLaNlBSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OlYzOzNpPkKzOFY3OjN|PD;hQi=>
Huh-luc/neo-ET replicon Mo\MRY51cX[rcnHsJIF{e2G7 NVTsVmpwPDhiaILz M2fhTWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BEKH[rcoXzJIdmdm:2eYDlJFFjKGmwIFj1bE1tfWNxbnXvMWVVKHKncHzpZ49vKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDy[ZBtcWOxbj3iZZNm\CCudXPp[oVz[XOnIHHzd4F6NCCHQ{WwQVAvODByMEJOwG0> NIfsUpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW2PFMyOyd-MkS1Olg{OTN:L3G+
HuH7 NUPibXBITnWwY4Tpc44h[XO|YYm= M4TjXGlvcGmkaYTpc44hd2ZiTmO1RUBqdiCKQ2[g[4Vvd3S7cHWtNYIhcW6oZXP0[YQhcW5iaIXtZY4hUHWKNzDj[YxteyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NE4xODByMkROwG0> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3M{ixNEc,OjV2NUO4NVA9N2F-
HuH7.5/Con1/SG-Neo(I)-hRluc2aUb M3PTVWZ2dmO2aX;uJIF{e2G7 MYK3NkBpenN? NUHmVIZ3UW6qaXLpeIlwdiCxZjDOV|VCKGmwIFjDWkBo\W6xdInw[UAy[iCrbn\lZ5Rm\CCrbjDoeY1idiCKdVi3MlUwS2:wMT;TS{1P\W9qSTmtbHJtfWN{YWXiJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZicnXwcIlkd25ibHX2[Yx{KGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF0xNjByMECyN:69VQ>? Mn7GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF5MUC0O|koRjNzN{GwOFc6RC:jPh?=
HuH7 MUDBcpRqfmm{YXygZZN{[Xl? NFXxNplCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJS1ZiZ3Xuc5R6eGViMXKgTmZJNTFiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wLDDFR|UxRTBwMECwNFI5|ryP NW[2WIxVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wO|c1QTNpPkK2NFc4PDl|PD;hQi=>
HuH7 M1q0VWFvfGm4aYLhcEBie3OjeR?= MXHBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3YhOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDifUBqdiC4aYTyc{Bz\XCuaXPvckBie3OjeTygSWM6OD1yLkCwNFA{|ryP NVnFRlNCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OlYzOzNpPkKzOFY3OjN|PD;hQi=>
HuH-Lcu-Neo NGnzO|RHfW6ldHnvckBie3OjeR?= NYHEe25UPDhiaILz NHruXlFKdmirYnn0bY9vKG:oIF7TOWEhcW5iSFPWJIdmdm:2eYDlJFFiKGmwZnXjeIVlKGmwIFj1TE1N[3VvTnXvJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC4aYLhcEBz\XCuaXPheIlwdiCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5yMECwN|I1|ryP M2qyNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzN{MkCyO|gzLz5|MkKwNlc5OjxxYU6=
HuH7 MXnBcpRqfmm{YXygZZN{[Xl? Mln4RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHX4dJJme3OrbnegUnM2SSCOM{HWJI12fGGwdDDpcoZm[3SnZDDpckBpfW2jbjDIeWg4KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjD2bZJidCCUTlGgdoVxdGmlYYTpc44tKEWFNUC9NE4xODByM{ZOwG0> NUjFfFJNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPVk2OzJpPkK2NFk6PTN{PD;hQi=>
Huh-luc/neo-ET replicon Ml3MRY51cX[rcnHsJIF{e2G7 NEDlOGY1QCCqcoO= M1XtemFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BEKH[rcoXzJIdmdm:2eYDlJFFiKGmwIFj1bE1tfWNxbnXvMWVVKHKncHzpZ49vKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDy[ZBtcWOxbj3iZZNm\CCudXPp[oVz[XOnIHHzd4F6NCCHQ{WwQVAvODByMEO5PO69VQ>? NWPTcJRpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1Olg{OTNpPkK0OVY5OzF|PD;hQi=>
HuH7 M4fXXGFvfGm4aYLhcEBie3OjeR?= MVnBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDD3bYxlKHS7cHWgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1TFch[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwII\pdoFtKFKQQTDy[ZBtcWOjdHnvckwhTUN3ME2wMlAxODB2ON88US=> NWL5VWFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPVk2OzJpPkK2NFk6PTN{PD;hQi=>
W11.8 NUjl[5dCSW62aY\pdoFtKGG|c3H5 MknEOEBl[Xm| MVLBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDI[ZBifGm2aYOgR{B3cXK3czDn[Y5wfHmyZTCxZUBqdm[nY4Tl[EBqdiCZMUGuPEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCQU{XBJIV5eHKnc4Ppc44hcW5icnXwcIlkd25iY3XscEBi\nSncjC0JIRigXNiYomgcJVucW6nc3PlcoNmKGKjc3XkJGVNUVODLDDFR|UxRTBwMECwNFXPxE1? M3izTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFEyLz5{NEmwNFgyOTxxYU6=
HuH7 NWiybGRKSW62aY\pdoFtKGG|c3H5 NED4XWI{KGSjeYO= NXPzeoN3SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHhJGg4PyCrbn\lZ5Rm\CCrbjDoeY1idiCKdVi3JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhWk6DIILldIxq[2G2aX;uJIFnfGW{IEOg[IF6eyCkeTDy[Y5qdGyjIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlAxODB3zszN NGHSS3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOyNFk{Oyd-MkSzNlA6OzN:L3G+
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HuH7 MVrBcpRqfmm{YXygZZN{[Xl? MYTBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhPWFiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5yMECwOVHPxE1? M3PQSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEWzPFEyLz5{NUS1N|gyOTxxYU6=
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GS4.3 MWnBcpRqfmm{YXygZZN{[Xl? M{nKe|AvOTVidV2= NXfNS5VbPiCmYYnz NVzvUlE1SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHnu[oVkfGWmIHnuJIh2dWGwIFfTOE4{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolz[WxiY3;y[UBxem:2ZXnuJIxmfmWuczDheEAxNjF3IIXNJJRz\WG2ZXSge4l1cCCocnXzbEBu\WSrYTDjc451[WmwaX7nJINwdXCxdX7kJIV3\XK7IEKg[IF6eyCvZXHzeZJm\CCjZoTldkA3KGSjeYOgZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ|MkW4Nkc,Ojl{M{K1PFI9N2F-
HuH7 Ml3TRY51cX[rcnHsJIF{e2G7 M33TUFMh\GG7cx?= NV3OXmE{SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHiJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[XRiPk2gNVAhfGmvZYOgZY51cX[rcnHsJGVEPTBiYX\0[ZIhOyCmYYnzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiYYPzZZk> NGjwbI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNFQ{Pyd-Mki0N|A1Ozd:L3G+
HuH7 NGjkdYtCdnSrdnnyZYwh[XO|YYm= MXWzJIRigXN? NVPQV2xRSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHiJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[29vdILlZZRm\CC5aYToJIF{fW6jcILleolzKGGodHXyJFMh\GG7czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGG|c3H5 NVzITGo6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|A1OzdpPkK4OFMxPDN5PD;hQi=>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[4]
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FRET assay for HCV NS5A inhibitors:

The peptide (Ac-Asp-Glu-Asp [EDANS]-Glu-Glu-Abu-[COO] Ala-Ser-Lys [DABCYL]-NH2) contains a fluorescence donor {EDANS, 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid} near one end of the peptide and an acceptor {DABCYL, 4-[(4-dimethylamino)phenyl]azo)benzoic acid} near the other end. Intermolecular resonance energy transfer between the donor and the acceptor quenches the fluorescence of the peptide, but as the NS3 protease cleaves the peptide, the products are released from resonance energy transfer quenching. The fluorescence of the donor increases over time as more substrate is cleaved by the NS3 protease. The assay reagent is: 5× luciferase cell culture lysis reagent diluted to 1× with dH2O, NaCl (150 mM), the FRET peptide (20 μM). HCV-Huh-7 cells are placed in a 96-well plate, and allowed to attach overnight (1×104 cells per well). The next day, BMS-790052 is added to the wells and the plate is incubated for 72 hours. The plate is then rinsed with PBS and used for the FRET assay by the addition of 30 μL of the FRET peptide assay reagent (described above) per well. Signals are obtained using the Cytofluor 4000 instrument, which has been set to 340 nm (excitation)/490 nm (emission) automatic mode, for 20 cycles or less, with the plate being read in the kinetic mode. Following FRET, 40 μL of luciferase substrate is added to each well and the luciferase is measured.
Cell Research:[1]
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  • Cell lines: HCV replicon cells (Huh7)
  • Concentrations: 0.1 pM - 50 μM, dissolved in DMSO (the final concentration of DMSO is 0.5%)
  • Incubation Time: 72 hours
  • Method: BMS-790052 is added to 96-well plates containing HCV replicon cells seeded approximately 12 hours before in 200 µL media.The cell plates are tested for replication activity and cytotoxicity after 72 hours of incubation. Cytotoxicity is measured with CellTiter-Blue, after which the media and dye are removed, plates are inverted and the remaining liquid is blotted with paper towels. Replication activity of the HCV genotype 1a cell lines is quantified using Renilla luciferase. 1× Renilla luciferase lysis buffer (30 µL) is added to each well and plates are incubated with gentle shaking for 15 min. Renilla luciferase substrate (40 µL) is then added and the signals are detected using a Top Count luminometer set for light emission quantification. One hundred per cent activity is calculated for each cell line for the DMSO-only wells; percentage activity is calculated for each concentration of the inhibitor by dividing the average value for wells containing compound by the average value for wells containing DMSO.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 148 mg/mL (200.3 mM)
Ethanol 148 mg/mL (200.3 mM)
Water 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.

Chemical Information

Molecular Weight 738.88
Formula

C40H50N8O6

CAS No. 1009119-64-5
Storage powder
in solvent
Synonyms EBP883
Smiles CC(C)C(C(=O)N1CCCC1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5=CN=C(N5)C6CCCN6C(=O)C(C(C)C)NC(=O)OC)NC(=O)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    C2
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04852614 Recruiting Diagnostic Test: Pharmacokinetic test Hepatitis C Virus Infection Ain Shams University December 1 2020 --
NCT04773756 Completed Drug: Sofosbuvir 400 MG/ Daclatasvir 60mg Covid19 Alexandria University November 1 2020 Phase 4
NCT03208322 Unknown status Other: Non-Interventional Hepatitis C Bristol-Myers Squibb November 30 2018 --
NCT03487848 Terminated Drug: Daclatasvir|Drug: Sofosbuvir Hepatitis C|Chronic Hepatitis Bristol-Myers Squibb June 25 2018 Phase 2
NCT03540212 Unknown status Drug: Daclatasvir and sofosbuvir Chronic HCV Infection Ain Shams University December 10 2017 Phase 2|Phase 3
NCT03004625 Completed Drug: daclatasvir|Drug: asunaprevir|Drug: Ribavirin Hepatitis C Kaohsiung Medical University Chung-Ho Memorial Hospital|Chang Gung Memorial Hospital|National Taiwan University Hospital|Taipei Veterans General Hospital Taiwan|China Medical University Hospital|National Cheng-Kung University Hospital November 2016 Phase 3

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.

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HCV Protease Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID