Product Name :
PF-3450074
Description:
PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
CAS:
1352879-65-2
Molecular Weight:
425.52
Formula:
C27H27N3O2
Chemical Name:
(2S)-N-methyl-2-[2-(2-methyl-1H-indol-3-yl)acetamido]-N,3-diphenylpropanamide
Smiles :
CC1NC2=CC=CC=C2C=1CC(=O)N[C@@H](CC1C=CC=CC=1)C(=O)N(C)C1C=CC=CC=1
InChiKey:
ACDFWSNAQWFRRF-VWLOTQADSA-N
InChi :
InChI=1S/C27H27N3O2/c1-19-23(22-15-9-10-16-24(22)28-19)18-26(31)29-25(17-20-11-5-3-6-12-20)27(32)30(2)21-13-7-4-8-14-21/h3-16,25,28H,17-18H2,1-2H3,(H,29,31)/t25-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.|Product information|CAS Number: 1352879-65-2|Molecular Weight: 425.52|Formula: C27H27N3O2|Chemical Name: (2S)-N-methyl-2-[2-(2-methyl-1H-indol-3-yl)acetamido]-N,3-diphenylpropanamide|Smiles: CC1NC2=CC=CC=C2C=1CC(=O)N[C@@H](CC1C=CC=CC=1)C(=O)N(C)C1C=CC=CC=1|InChiKey: ACDFWSNAQWFRRF-VWLOTQADSA-N|InChi: InChI=1S/C27H27N3O2/c1-19-23(22-15-9-10-16-24(22)28-19)18-26(31)29-25(17-20-11-5-3-6-12-20)27(32)30(2)21-13-7-4-8-14-21/h3-16,25,28H,17-18H2,1-2H3,(H,29,31)/t25-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (587.{{AK-1} site|{AK-1} Epigenetics|{AK-1} Protocol|{AK-1} In Vitro|{AK-1} supplier|{AK-1} Epigenetics} 52 mM; Need ultrasonic).{{DMBA} medchemexpress|{DMBA} Purity & Documentation|{DMBA} Purity|{DMBA} supplier|{DMBA} Epigenetics} |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:23800738 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|PF-3450074 (PF-74) exhibits anti-viral activities against HIV wild type NL4-3 and HIV T107N mutant with EC50 values of 0.72 μM and 4.5μM, respectively. PF-3450074 (PF-74) displays a good potency in primary human peripheral blood mononuclear cells (PBMCs), inhibits HIV-193RW025, HIV-1JR-CSF and HIV-193MW965 with IC50 values of 1.5 ± 0.9 μM; 0.6 ± 0.20 μM; and 0.6 ± 0.10 μM, respectively. This compound shows Median IC50 and CC50 values of 0.9 ± 0.5 μM and 90.5 ± 5.9 μM, respectively. The KD for the interaction between PF-74 and the CA hexamer, derived in the same manner as for NUP153, is determined to be 176 ± 78 nM. PF-3450074 (PF-74) (10 μM; 8 hours) results in a marked reduction in late products of reverse transcription in HeLa-P4 cells with DNase I-treated stocks of Env-defective HIV-1 (R9.Env-).|Products are for research use only. Not for human use.|
