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AdipoGen Life Sciences
Nelfinavir . mesylate
60
CHF
CHF 60.00
In stock
AG-CR1-3726-M01010 mgCHF 60.00
AG-CR1-3726-M05050 mgCHF 240.00
| Product Details | |
|---|---|
| Synonyms | AG-1343; Nelfin; Viracept |
| Product Type | Chemical |
| Properties | |
| Formula |
C32H45N3O4S . CH4SO3 |
| MW | 567.8 . 96.1 |
| CAS | 159989-65-8 |
| RTECS | NW6995333 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (15mg/ml), DMF (20mg/ml) or ethanol (20mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | NQHXCOAXSHGTIA-SKXNDZRYSA-N |
| Smiles | O[C@@H]([C@H](CSC1=CC=CC=C1)NC(C2=C(C)C(O)=CC=C2)=O)CN3C[C@@]4([H])CCCC[C@@]4([H])C[C@H]3C(NC(C)(C)C)=O.CS(=O)(O)=O |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Nelfinavir is an orally bioavailable competitive inhibitor of the human immunodeficiency virus. It potently inhibits HIV-1 (Ki=2nM) and HIV-2 protease in vitro. HIV-1 protease is important for the replication of the virus within the cell and the release of mature viral particles from the infected cell.
- Formulations containing nelfinavir have been used in combination with HIV reverse transcriptase inhibitors for the treatment of AIDS.
- Nelfinavir shows other antimicrobial and antiviral activity. It inhibits maturation and export of the Herpes Simplex 1 virus and the Kaposi's Sarcoma virus, replication of SARS-CoV and also replication of SARS-CoV-2, cause for the epidemic COVID-19.
- Has potent anti-cancer activity against a broad selection fo cancer cell types. Shown to induce apoptosis, autophagy, cell cycle arrest and endoplasmic reticulum stress, which consequently leads to cancer cell death. Shown to inhibit the Akt/PKB signaling pathway.
- It acts as an antifibrotic agent and is used to treat pulmonary fibrosis in patients with systemic sclerosis (SSc) and reduces inflammation by activating protein phosphatase 2 (PP-2) and blocking mitogen-activated protein kinases (MAPK) signaling in macrophages.
- It has also shown pan-proteasome inhibition in AMO-1 and U266 myeloma cells.
Product References
- Viracept (nelfinavir mesylate, AG1343): A potent, orally bioavailable inhibitor of HIV-1 protease: S.W. Kaldor, et al.; J. Med. Chem. 40, 3979 (1997)
- Nelfinavir mesylate: a protease inhibitor: V.B. Pai & M.C. Nahata; Ann. Pharmacother. 33, 325 (1999) (Review)
- HIV protease inhibitor nelfinavir inhibits replication of SARS-associated coronavirus: N. Yamamoto, et al.; BBRC 318, 719 (2004)
- The HIV protease inhibitors saquinavir, ritonavir, and nelfinavir induce apoptosis and decrease barrier function in human intestinal epithelial cells: H. Bode, et al.; Antivir. Ther. 10, 645 (2005)
- HIV protease inhibitor nelfinavir inhibits growth of human melanoma cells by induction of cell cycle arrest: W. Jiang, et al.; Cancer Res. 67, 1221 (2007)
- The HIV protease inhibitor nelfinavir downregulates Akt phosphorylation by inhibiting proteasomal activity and inducing the unfolded protein response: A.K. Gupta, et al.; Neoplasia 9, 271 (2007)
- Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that induces endoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo: J.J. Gills, et al.; Clin. Cancer Res. 13, 5183 (2007)
- New prospects for nelfinavir in non-HIV-related diseases: A. Bruning, et al.; Curr. Mol. Pharmacol. 3, 91 (2010) (Review)
- Nelfinavir, an HIV-1 protease inhibitor, induces oxidative stress-mediated, caspase-independent apoptosis in Leishmania amastigotes: P. Kumar, et al.; PLoS Negl. Trop. Dis. 4, e642 (2010)
- The HIV protease inhibitor nelfinavir inhibits Kaposi's sarcoma-associated herpesvirus replication in vitro: S. Gantt, et al.; Antimicrob. Agents Chemother. 55, 2696 (2011)
- The HIV-1 protease inhibitor nelfinavir activates PP2 and inhibits MAPK signaling in macrophages: a pathway to reduce inflammation: M.A. Wallet, et al.; J. Leukoc. Biol. 92, 795 (2012)
- Selective inhibition of HER2-positive breast cancer cells by the HIV protease inhibitor nelfinavir: J.S. Shim, et al.; J. Natl. Cancer Inst. 104, 1576 (2012)
- The human immunodeficiency virus-1 protease inhibitor nelfinavir impairs proteasome activity and inhibits the proliferation of multiple myeloma cells in vitro and in vivo: C. Bono, et al.; Haematologica 97, 1101 (2012)
- Nelfinavir impairs glycosylation of herpes simplex virus 1 envelope proteins and blocks virus maturation: S. Gantt, et al.; Adv. Virol. 2015, 687162 (2015)
- Systemic sclerosis: Antiviral drug inhibits lung fibrosis: J. McHugh; Nat. Rev. Rheumatol. 13, 696 (2017) (Review)
- Nelfinavir is active against SARS-CoV-2 in Vero E6 cells: Z. Xu, et al.; ChemRxiv (Preprint) (2020)
- Nelfinavir inhibits replication of severe acute respiratory syndrome coronavirus 2 in vitro: N. Yamamoto, et al.; BioRxiv (Preprint) (2020)
- Nelfinavir was predicted to be a potential inhibitor of 2019-nCov main protease by an integrative approach combining homology modelling, molecular docking and binding free energy calculation: Z. Xu, et al.; BioRxiv (Preprint) (2020)
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