1. Metabolic Enzyme/Protease
    Anti-infection
  2. HIV Protease
    HIV
  3. Nelfinavir

Nelfinavir (Synonyms: AG1341)

Cat. No.: HY-15287 Purity: 98.16%
Handling Instructions

Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.

For research use only. We do not sell to patients.

Nelfinavir Chemical Structure

Nelfinavir Chemical Structure

CAS No. : 159989-64-7

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10 mM * 1 mL in DMSO Get quote
5 mg USD 144 Get quote
10 mg USD 240 Get quote
50 mg USD 672 Get quote

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Description

Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2] Target: HIV Protease in vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2]. in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (44.03 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7612 mL 8.8062 mL 17.6125 mL
5 mM 0.3522 mL 1.7612 mL 3.5225 mL
10 mM 0.1761 mL 0.8806 mL 1.7612 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

567.78

Formula

C₃₂H₄₅N₃O₄S

CAS No.

159989-64-7

SMILES

[H][[email protected]]12C[[email protected]@H](C(NC(C)(C)C)=O)N(C[[email protected]]([[email protected]@H](NC(C3=C(C)C(O)=CC=C3)=O)CSC4=CC=CC=C4)O)C[[email protected]@]1([H])CCCC2

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Room temperature in continental US; may vary elsewhere

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Nelfinavir

Cat. No.: HY-15287