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Purity: ≥98%
PF-3450074 (also known as PF74) is a HIV-1 capsid-targeting small molecule antiviral compound which directly binds to the capsid (CA) protein at a site also utilized by host cell proteins CPSF6 and NUP153. The RNA genome of human immunodeficiency virus type 1 (HIV-1) is enclosed in a cone-shaped capsid shell that disassembles following cell entry via a process known as uncoating. During HIV-1 infection, the capsid is important for reverse transcription and entry of the virus into the target cell nucleus. The small molecule PF74 inhibits HIV-1 infection at early stages by binding to the capsid and perturbing uncoating.
| Targets |
NL4.3 strain（IC50=0.72 μM）
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|---|---|
| ln Vitro |
PF-3450074, also known as PF-74, demonstrates antiviral properties against the HIV T107N mutant and HIV wild type NL4-3, with EC50 values of 4.5μM and 0.72μM, respectively[1].
In primary human peripheral blood mononuclear cells (PBMCs), PF-3450074 (PF-74) exhibits good potency, inhibiting 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. The median IC50 and CC50 values for this compound are 0.9 ± 0.5 μM and 90.5 ± 5.9 μM, respectively[1]. Derived similarly to NUP153, the KD for the interaction between PF-74 and the CA hexamer is found to be 176 ± 78 nM[1]. PF-3450074 (PF-74) (10 μM; 8 hours) significantly lowers the late products of reverse transcription in stocks of DNase I-treated Env-defective HIV-1 (R9.Env-) in HeLa-P4 cells[2]. |
| Cell Assay |
Cell Line: HeLa-P4 cells
Concentration: 10 μM Incubation Time: 8 hours Result: prevented target cells from undergoing HIV-1 reverse transcription. |
| References |
| Molecular Formula |
C27H27N3O2
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|---|---|
| Molecular Weight |
425.53
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| Exact Mass |
425.21
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| Elemental Analysis |
C, 76.21; H, 6.40; N, 9.87; O, 7.52
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| CAS # |
1352879-65-2
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| Related CAS # |
1352879-65-2;
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| Appearance |
Solid powder
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| SMILES |
O=C(N[C@@H](CC1=CC=CC=C1)C(N(C)C2=CC=CC=C2)=O)CC3=C(C)NC4=C3C=CC=C4
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| InChi Key |
ACDFWSNAQWFRRF-VWLOTQADSA-N
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| InChi Code |
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
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| Chemical Name |
2-Methyl-N-[(1S)-2-(methylphenylamino)-2-oxo-1-(phenylmethyl)ethyl]- 1H-indole-3-acetamide
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| Synonyms |
PF74; PF-74; PF 74; PF-3450074; PF 3450074; PF3450074;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~587.52 mM）
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (14.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 2: 10% DMSO+90% Corn Oil: ≥ 6.25 mg/mL (14.69 mM) (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3500 mL | 11.7501 mL | 23.5001 mL | |
| 5 mM | 0.4700 mL | 2.3500 mL | 4.7000 mL | |
| 10 mM | 0.2350 mL | 1.1750 mL | 2.3500 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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