LY411575

製品コードS2714

LY411575化学構造

分子量(MW):479.48

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells.

サイズ 価格(税別)  
JPY 56440.00
JPY 28220.00
JPY 53120.00
JPY 161020.00

カスタマーフィードバック(1)

  • (E) Quantitation of lumen from A-D. (F) RNA isolated from 6d acini and expression of NOTCH1 measured by qRT-PCR in triplicate. P values are * <.01, *** <0.001.

    Exp Cell Res, 2017, 359(2):384-393. LY411575 purchased from Selleck.

製品安全説明書

Gamma-secretase阻害剤の選択性比較

生物活性

製品説明 LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells.
ターゲット
γ secretase (membrane-based) [1]
(HEK293 cells expressing either APP or NΔE)
γ secretase (cell-based) [1]
(HEK293 cells expressing either APP or NΔE)
Notch S3 cleavage [1]
(HEK293 cells expressing either APP or NΔE)
0.078 nM 0.082 nM 0.39 nM
体外試験

LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage. [1] LY-411575, which blocks Notch activation, results in apoptosis in primary and immortalized KS cells. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells M2fpOmZ2dmO2aX;uJIF{e2G7 Mn7DTY5pcWKrdHnvckBw\iCpYX3tZUB{\WO{ZYThd4UhcW5iaIXtZY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJIFugWyxaXSgZoV1[SB2MDDwdo9lfWO2aX;uMEBGSzVyPUCuNFAxOTF7IN88US=> NGfrSVUyPzV5M{O0Oi=>
CHO cells MlzGSpVv[3Srb36gZZN{[Xl? MoH3NlQhcA>? NVOyVoJzWmWmdXP0bY9vKG:oIHj1cYFvKFCVMTDk[Yx1[SCneH;uPUBufXSjboStbY5lfWOnZDDhcZltd2mmIHLleIEuPDJibHX2[YwhcW5iQ1jPJINmdGy|IH;2[ZJmgHC{ZYPzbY5oKGi3bXHuJGFRWDd3MXHmeIVzKDJ2IHjyd{BjgSCuaYH1bYQheGijc3Wg[Yxm[3S{b3Po[Y1qdHWvaX7ld4NmdmOnIHHzd4F6KHKnbHH0bZZmKHSxIHPvcpRzd2xuIFXDOVA:OC5yMECzOVIh|ryP NY[5O4gxOTd3N{OzOFY>
CHO cells M1\YV2Z2dmO2aX;uJIF{e2G7 M1HGOlI1KGh? MYTS[YR2[3Srb36gc4YhcHWvYX6gVHMyKGSnbIThJIV5d257IH31eIFvfC2rbnT1Z4VlKGGveXzvbYQh[mW2YT20NEBt\X[nbDDpckBEUE9iY3XscJMhd3[ncnX4dJJme3OrbnegbJVu[W5iQWDQO|Uy[W[2ZYKgNlQhcHK|IHL5JIxqeXWrZDDwbIF{\SCnbHXjeJJw[2inbXnseY1qdmW|Y3XuZ4Uh[XO|YYmgdoVt[XSrdnWgeI8h[2:wdILvcC=> NXPuRYx2OTd3N{OzOFY>
CHO cells Mn\mSpVv[3Srb36gZZN{[Xl? MnTpNlQhcA>? M1LCXnJm\HWldHnvckBw\iCqdX3hckB4cWymIIT5dIUhWFNzLXnu[JVk\WRiYX35cI9q\CCkZYThMVQxKGyndnXsJIlvKEOKTzDj[YxteyCxdnXy[ZhxemW|c3nu[{BpfW2jbjDBVHA4PTFiYX\0[ZIhOjRiaILzJIJ6KGyrcYXp[EBxcGG|ZTDlcIVkfHKxY3jlcYltfW2rbnXzZ4Vv[2ViYYPzZZkhemWuYYTpeoUhfG9iY3;ueJJwdCxiRVO1NF0xNjByMEGxOEDPxE1? MWGxO|U4OzN2Nh?=
CHO cells NXvVU5hvTnWwY4Tpc44h[XO|YYm= NFfjSG8zPCCq NVuyXIh1WmWmdXP0bY9vKG:oIHj1cYFvKHerbHSgeJlx\SCSU{GtbY5lfWOnZDDhcZltd2mmIHLleIEuPDJibHX2[YwhcW5iQ1jPJINmdGy|IH;2[ZJmgHC{ZYPzbY5oKGi3bXHuJGFRWDd3MTDh[pRmeiB{NDDodpMh[nlibHnxeYllKHCqYYPlJIVt\WO2cn;jbIVucWy3bXnu[ZNk\W6lZTDhd5NigSC{ZXzheIl3\SC2bzDjc451em:uLDDFR|UxRTBwMECwNVM2KM7:TR?= NUfodolkOTd3N{OzOFY>
SH-SY5Y cells MYXGeY5kfGmxbjDhd5NigQ>? MmixTY5pcWKrdHnvckBw\iCpYX3tZUB{\WO{ZYThd4UudWWmaXH0[YQh[W27bH;p[EBj\XSjIDixJJRwKDRyKTDwdo9lfWO2aX;uJIlvKGi3bXHuJHNJNVO\NWmgZ4VtdHNuIFnDOVA:OC5yMEGg{txO MXuxPVY6PDR4Nx?=
H4 cells NWDtfmN7TnWwY4Tpc44h[XO|YYm= NIP4XIkyODBibl2= NYf6UGVUOTZiaB?= M2r4ZWlvcGmkaYTpc44hd2ZiZ3HtcYEhe2WlcnX0ZZNmKGW6cILld5Nm\CCrbjDoeY1idiCKNDDj[YxteyCneIDy[ZN{cW6pIFLSTU1EQTliZoXzbY9vKHC{b4TlbY4h[XO|ZYPz[YQh[XNiQ{m5JIZz[WevZX70JIFk[3WvdXzheIlwdiCocnHncYVvfCCjdDCxNFAhdk1iaX7jeYJifGWmIH\vdkAyPiCqcoOgbY4h[nliaX3teY5w[myxdB?= MWSyN|E5OTVyMh?=
H4 cells NHrDeVRHfW6ldHnvckBie3OjeR?= MkjMNVAxKG6P NGDpV4UyPiCq NF:xRY5KdmirYnn0bY9vKG:oIHfhcY1iKHOnY4LleIF{\SCneIDy[ZN{\WRiaX6gbJVu[W5iSESgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEN6MzDs[ZZmdHNiYYSgNVAhfU1iaX7jeYJifGWmIH\vdkAyPiCqcoOgZpkhcW2vdX7vZoxwfA>? MmXUNlMyQDF3MEK=
H4 cells NYPHcXRRTnWwY4Tpc44h[XO|YYm= M3rCOFExKHWP M3r3eFE3KGh? NYLBeWpHUW6qaXLpeIlwdiCxZjDnZY1u[SC|ZXPy[ZRie2ViZYjwdoV{e2WmIHnuJIh2dWGwIFi0JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCFVF[gcIV3\Wy|IHH0JFExKHWPIHnuZ5Vj[XSnZDDmc5IhOTZiaILzJIJ6KGmvbYXuc4Jtd3R? NF7IbJYzOzF6MUWwNi=>
HEK293 cells MUDGeY5kfGmxbjDhd5NigQ>? MXizJIRigXN? MoDJUY9lfWyjdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iSFXLNlk{KGOnbHzzJIV5eHKnc4Ppcoch\3WrbnXhJJBq\yCVd3XkbZNpKG23dHHueEBUTlZvQWDQOlk2e3diY3;lfJBz\XO|aX7nJGRNVDRiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCwb4TjbEBxem:lZYPzbY5oKGmwIHj1cYFvKFSHNkexJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCmdXHsMYNmdGxibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUGuNkDPxE1? NEjFcVIzPDF|OUW4Ny=>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 10 mg/kg oral dose of LY-411575 decreases brain and plasma Aβ40 and -42 dose-dependently. [1] LY-411575 reduces cortical Aβ40 in young (preplaque) transgenic CRND8 mice (ED50 ≈ 0.6 mg/kg) and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg). The therapeutic window is similar after oral and subcutaneous administration and in young and aged CRND8 mice. Both the thymus and intestinal side effects are reversible after a 2-week washout period. Three-week treatment with 1 mg/kg LY411575 reduces cortical Aβ40 by 69% without inducing intestinal effects, although a previously unreported change in coat color is observed. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

Assays for Aβ and NICD:

Procedures for measuring γ-secretase activity in membranes prepared from HEK293 cells expressing APP have been described previously (Zhang L et al Biochemistry 40, 5049-5055). Intact HEK293 cells expressing either APP or NΔE are treated with various concentrations of LY- 411,575 for 4 hours at 37 °C. In the case of cells expressing NΔE, cells are lysed, the cell lysates are separated on a 4-12% NuPAGE gel, and the processed NICD fragment is detected via Western blot with a cleavage site-specific antibody. The inhibition of NICD production is quantified by spot densitometric analysis using FluorChem. In the case of cells expressing APP, the conditioned medium is collected, centrifuged at 10,000 × g for 5 minutes to remove cell debris, and stored at -20 °C prior to the determination of Aβ levels. Aβ40 and -42 produced in HEK293 membrane- and cell-based assays, as well as plasma Aβ40 and cortex Aβ40 from TgCRND8 mice, are analyzed without pretreatment using an electrochemiluminescence detection-based immunoassay. Plasma Aβ42 is measured by enzyme-linked immunosorbent assay. A commercially available enzyme-linked immunosorbent assay kit is used to measure cortex Aβ42 according to the manufacturer''s instructions.
細胞試験:

[2]

+ 展開
  • 細胞株: primary and immortalized KS cells
  • 濃度: 500 μM
  • 反応時間: 24 hours
  • 実験の流れ:

    DNA/PI staining is performed using standard methodologies. Briefly, 1 × 106 cells are permeabilized with 100% ethanol in the presence of 15% FBS. The cells are washed and then treated for 15 minutes at 37 °C with 10 mg/mL RNAse. PI (5 mg/mL) is added, and the cells incubated for 1 hour at 4 °C prior to analysis by flow cytometry with 10 000 cells analysed per gated determination. The results are confirmed using the Immunotech Annexin V staining kit following the manufacturers’ instructions. At least three independent experiments are performed showing similar results.(参考用のみ)

動物試験:

[1]

+ 展開
  • 動物モデル: TgCRND8 mice model
  • 製剤: LY-411575 is formulated as 10 mg/mL solutions in 50% polyethylene glycol, 30% propylene glycol, 10% ethanol and diluted in 0.4% methylcellulose for dosing.
  • 投薬量: 1-10 mg/kg
  • 投与方法: Orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 95 mg/mL (198.13 mM)
Ethanol 13 mg/mL (27.11 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% PEG400+0.5% Tween80+5% propylene glycol
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 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 479.48
化学式

C26H23F2N3O4

CAS No. 209984-57-6
保管
in solvent
別名 N/A

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 (g) = 濃度 (mol/L) x 体積 (L) 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MSDS/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MSDS/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

よくある質問(FAQ)

  • 質問1:

    Does this inhibitor act on beta-secretase?.

  • 回答:

    LY411575 has been reported to inhibit gamma-secretase, currently, there is no publication reporting its inhibition on beta-secreatse.

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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