Nelfinavir (AG 1343) Mesylate

For research use only. Not for use in humans.

製品コードS4282 別名:Viracept

Nelfinavir (AG 1343) Mesylate化学構造

CAS No. 159989-65-8

Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.

サイズ 価格(税別)  
JPY 24700
JPY 100900
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バルク問合せ

製品安全説明書

HIV Protease阻害剤の選択性比較

生物活性

製品説明 Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.
ターゲット
HIV protease [1]
(Cell-free assay)
2 nM(Ki)
細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Saos-2 NUmwRXNreUiWUzDhd5NigQ>? NV\OUWZWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> NWTKb4l6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NH3tRpRyUFSVIHHzd4F6 M{\BcZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD MYnxTHRUKGG|c3H5 NEjtUJhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? NILaem89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) MXvxTHRUKGG|c3H5 M3LQe5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MT2 M4D4SGFvfGm4aYLhcEBie3OjeR?= MX61JIRigXN? MlLlRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4Sge4lt\CC2eYDlJGhKXjFiM1KgbY5n\WO2ZXSgbY4hcHWvYX6gUXQzKGOnbHzzJIF{e2W|c3XkJIF{KH[rcoXzMYlv\HWlZXSgZ5l1d3CjdHjpZ{Bm\m[nY4SgZYZ1\XJiNTDkZZl{KGK7IGjUWEBie3OjeTygSWM2OD1yLkCwOFnPxE1w MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1PFQwLz6FaFXNRmw9N2F-
HepG2 Mn:4R5l1d3SxeHnjbZR6KGG|c3H5 Mke4OUBl[Xm| MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPSCmYYnzJIJ6KFiWVDDhd5NigSxiQ1O1NF04NjUQvF2u MnjxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVg1Nyd-Q3jFUWJNRC:jPh?=
skeletal myoblast cells NYLsb3dPS3m2b4TvfIlkcXS7IHHzd4F6 NIX6NZU4OiCqb4Xydy=> NYX5bm1KTE6GSUqgR5l1d3SxeHnjbZR6KGmwIG\peJJwNCB5MjDoc5VzNCCrbjDyZZQhe2unbHX0ZYwhdXmxYnzhd5Qh[2WubIOsJGlEPTB;MUKuNFXPxE1w Mm\LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVg1Nyd-Q3jFUWJNRC:jPh?=
MT2 M3\oUGN6fG:2b4jpZ4l1gSCjc4PhfS=> NX;wS3F6PSCmYYnz MlnkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXQzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA2KGSjeYOgZpkhYFSWIHHzd4F6NCCFQ{WwQVE6NjIQvF2u NVPHc|l3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTh2Lze+R4hGVUKOPD;hQi=>

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アッセイ
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 22271897     


Histograms show the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines treated with nelfinavir (1 μM to 10 μM).

22271897
Western blot
p-eIF2Aα / eIF2Aα / ATF4 / GRP78 / CHOP ; 

PubMed: 21697087     


U251 cells were mock-treated (0) or treated with Nelfinavir (NFV) (20 μm) for 4 or 24 h then whole cell lysates were immunoblotted for P-eIF2α, eIF2α, ATF4, GRP78, CHOP, and Ran, as indicated. 

SOD1 / SOD2 / catalase ; 

PubMed: 27280849     


Protein lysates derived from MDA-MB231, MCF-7, or breast epithelial cells, treated with 10 μM nelfinavir for the indicated time points, were immunoblotted with anti- SOD1, anti-SOD2 and anti-catalase. Beta-actin was used as loading control. 

PAX3 / MITF ; 

PubMed: 26977879     


Western blot of the indicated cell lines treated with 10 μM nelfinavir for 24 hr for PAX3, MITF, and ERK2.

21697087 27280849 26977879
Immunofluorescence
LC3 / p62 ; 

PubMed: 27330277     


Immunofluorescence of cells treated with control 0.1% dimethyl sulfoxide or 10 μM nelfinavir for 24 hours. Scale bars indicate 10 μm and apply to all images. Punctate LC3 were quantified as autophagosomes and punctate p62 were quantified as sequestosomes, **P<0.01, ***P<0.001. (C and D) Western blot of lysates prepared following 24 hours of drug treatment. Nelfinavir was used at 10 μM and the autophagy clearance inhibitor chloroquine at 10 μM. 

PAX3 / MITF ; 

PubMed: 26977879     


Immunofluorescence analysis for PAX3 and MITF in WM266-4 cells left untreated or treated with 10 μM nelfinavir for 24 hr; scale bars, 50 μm.

p-SMAD2 ; 

PubMed: 26977879     


Immunofluorescence analysis for phospho-SMAD2 in melanoma cells treated with nelfinavir; scale bars, 10 μm

27330277 26977879
体内試験 In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. Initial investigation of the compound in fed rats indicated an oral bioavailability of 43%. In contrast, the oral bioavailability was significantly reduced in fasted rats to 29%. Nelfinavir demonstrated significant oral bioavailabilability across a range of species including dogs (47%), marmosets (17%), and cynomolgus monkeys (26%). It has a long plasma half-life after oral dosing that is likely due to a combination of slow dissolution and absorption. nelfinavir is well absorbed in humans particularly when administered with food and possesses minimal and easily managed side effects[1].

お薦めの試験操作(参考用のみ)

動物試験:

[1]

- 合併
  • 動物モデル: Sprague-Dawley rats
  • 投薬量: 12.5 to 25 mg/kg (i.v); 25 to 50 mg/kg (oral)
  • 投与方法: i.v and oral administration
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (150.62 mM)
Water Insoluble
Ethanol ''100 mg/mL ''100

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 663.89
化学式

C33H49N3O7S2

CAS No. 159989-65-8
Storage powder
in solvent
別名 Viracept
Smiles CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O.CS(=O)(=O)O

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

HIV Proteaseシグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID