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PZ0013

Sigma-Aldrich

Nelfinavir mesylate hydrate

≥98% (HPLC)

Sinonimo/i:

3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide methanesulfonate, AG-1343, Nelfinavir methanesulfonate hydrate

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About This Item

Formula empirica (notazione di Hill):
C32H45N3O4S · CH3SO3H · xH2O
Numero CAS:
Peso molecolare:
663.89 (anhydrous basis)
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77
Prezzi e disponibilità al momento non sono disponibili

Saggio

≥98% (HPLC)

Stato

powder

Colore

white to off-white

Solubilità

DMSO: ≥2 mg/mL

Temperatura di conservazione

2-8°C

Stringa SMILE

CC1=C(O)C=CC=C1C(N[C@@H](CSC2=CC=CC=C2)[C@H](O)CN3[C@H](C(NC(C)(C)C)=O)C[C@@]4([H])[C@@](CCCC4)([H])C3)=O.[CH2]S(O)(=O)=O

InChI

1S/C32H45N3O4S.CH4O3S/c1-21-25(15-10-16-28(21)36)30(38)33-26(20-40-24-13-6-5-7-14-24)29(37)19-35-18-23-12-9-8-11-22(23)17-27(35)31(39)34-32(2,3)4;1-5(2,3)4/h5-7,10,13-16,22-23,26-27,29,36-37H,8-9,11-12,17-20H2,1-4H3,(H,33,38)(H,34,39);1H3,(H,2,3,4)/t22-,23+,26-,27-,29+;/m0./s1
NQHXCOAXSHGTIA-SKXNDZRYSA-N

Applicazioni

Nelfinavir mesylate hydrate has been used to test its therapeutic effect on pulmonary fibrosis in patients with systemic sclerosis (SSc).[1] It has also been used in combination with bortezomib to selectively kill tuberous sclerosis complex 2 (TSC2)-deficient tumor cells.[2]

Azioni biochim/fisiol

Nelfinavir is a HIV protease inhibitor; antiretroviral; and anti-tumor agent.
Nelfinavir mesylate hydrate, also known as AG1343, is used as a therapeutic agent for acquired immunodeficiency syndrome (AIDS).[3] It acts as an antifibrotic agent and is used to treat pulmonary fibrosis in patients with systemic sclerosis (SSc). In addition, nelfinavir mesylate hydrate reduces inflammation by activating protein phosphatase 2 (PP-2) and blocking mitogen-activated protein kinases (MAPK) signaling in macrophages. It also stimulate autophagy and exhibit anti-cancer property.[1]

Caratteristiche e vantaggi

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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Loss of tuberous sclerosis complex 2 sensitizes tumors to nelfinavir- bortezomib therapy to intensify endoplasmic reticulum stress-induced cell death
Johnson C, et al.
Oncogene, 37(45), 5913-5913 (2018)
Saneesh Kumar et al.
Frontiers in pharmacology, 11, 517-517 (2020-05-20)
Ocimum basilicum L. or basilicum is a common culinary herb, used as a traditional medicine for various medical conditions including HIV/AIDS and tuberculosis, in Africa. The objective of this study was to evaluate the effect of methanol, ethanol, aqueous and
S Kawabata et al.
Cell death & disease, 3, e353-e353 (2012-07-25)
Exploiting protein homeostasis is a new therapeutic approach in cancer. Nelfinavir (NFV) is an HIV protease inhibitor that induces endoplasmic reticulum (ER) stress in cancer cells. Under conditions of ER stress, misfolded proteins are transported from the ER back to
Camille Bono et al.
Haematologica, 97(7), 1101-1109 (2012-01-25)
Multiple myeloma is characterized by the accumulation of tumor plasma cells in the bone marrow. Despite therapeutic improvements brought by proteasome inhibitors such as bortezomib, myeloma remains an incurable disease. In a variety of human cancers, human immunodeficiency virus protease
Karin Nielsen-Saines et al.
The New England journal of medicine, 366(25), 2368-2379 (2012-06-22)
The safety and efficacy of adding antiretroviral drugs to standard zidovudine prophylaxis in infants of mothers with human immunodeficiency virus (HIV) infection who did not receive antenatal antiretroviral therapy (ART) because of late identification are unclear. We evaluated three ART

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Bioactive small molecules for immune system signaling target identification/validation and antibiotics, antivirals, and antifungals offered.

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