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

Nelfinavir Mesylate (Synonyms: AG 1343 Mesylate)

製品番号: HY-15287A 純度: 99.02%
取扱説明書

Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.

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Nelfinavir Mesylate 構造式

Nelfinavir Mesylate 構造式

CAS 番号 : 159989-65-8

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 88 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 60 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 79 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 192 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 282 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 444 在庫あり
Estimated Time of Arrival: December 31
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 6 publication(s) in Google Scholar

Other Forms of Nelfinavir Mesylate:

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製品説明

Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent[1][2][3].

IC50 & Target[1]

HIV-1

 

体外実験

Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells[4].
Nelfinavir Mesylate inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells[4].
Nelfinavir Mesylate (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines[4].
Nelfinavir Mesylate (5 μM; 0-24 hours) decreases the phosphorylation of AKT[4].
Nelfinavir Mesylate activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system[4].

Cell Proliferation Assay[4]

Cell Line: RPMI, LP1, U266, OPM2 and MM1S cells
Concentration: 1, 2, 5, 10 μM
Incubation Time: 48 hours
Result: Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC50 of 1-5 μM.

Apoptosis Analysis[4]

Cell Line: LP1 and U266 cells
Concentration: 1-10 μM
Incubation Time: 17 hours
Result: Induced a dose-dependent increase in the percentage of annexin V+/propidium iodide+ cells.

Western Blot Analysis[4]

Cell Line: U266 cells
Concentration: 5 μM
Incubation Time: 0-24 hours
Result: The level of AKT phosphorylation in U266 cells decreased.
体内実験

Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice[4].

Animal Model: NOD/SCID mice (bearing U266-luc cells)[4]
Dosage: 75 mg/kg
Administration: I.p.; 5 days a week for 21 days
Result: Decreased MM cell growth in NOD/SCID mice.
臨床実験
分子量

663.89

分子式

C₃₃H₄₉N₃O₇S₂

CAS 番号

159989-65-8

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.CS(=O)(O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 25 mg/mL (37.66 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5063 mL 7.5314 mL 15.0627 mL
5 mM 0.3013 mL 1.5063 mL 3.0125 mL
10 mM 0.1506 mL 0.7531 mL 1.5063 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.77 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献

純度: 99.02%

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Keywords:

NelfinavirAG 1343AG1343AG-1343HIV ProteaseHIVHuman immunodeficiency virusproteaseproliferationmultiplemyelomacellsphosphorylationNOproductioninfectionInhibitorinhibitorinhibit

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製品名:
Nelfinavir Mesylate
製品番号:
HY-15287A
数量:
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