Nelfinavir (Mesylate)
产品编号: DC9474
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应用领域
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.
| Cas No.: |
159989-65-8 |
| 名称: |
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| 别名: |
AG 1343 Mesylate;AG1343 Mesylate;AG-1343 Mesylate |
| SMILES: |
OS(=O)(C)=O.O=C([C@H]1N(C[C@@H](O)[C@@H](NC(C2=CC=CC(O)=C2C)=O)CSC3=CC=CC=C3)C[C@@]4([H])CCCC[C@@]4([H])C1)NC(C)(C)C |
| 分子式: |
C33H49N3O7S2 |
| 分子量: |
663.888 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| References: |
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.
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. 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.
in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. |
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MSDS
COA
| LOT NO. |
DOWNLOAD |
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| 2018-0101 |
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