Fingolimod (FTY720) HCl 化学構造
分子量: 343.9

高品質保証

カスタマーフィードバック(3)

Quality Control & MSDS

製品説明

  • Compare S1P Receptor Inhibitors
    S1P Receptor製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Fingolimod (FTY720) HCl(フィンゴリモド、Gilenya)は、0.033nMのIC50によるスフィンゴシン1-リン酸(S1P)受容体拮抗剤です。
ターゲット S1P receptor
IC50 0.033 nM [1]
In vitro試験 The inhibitory effect of S1P is revered by various concentrations of FTY720, with IC50 effect of 173 nM. In addition, FTY720 (10 nM) alone exerts no effect on the expression of co-stimulatory molecules. FTY720 reverses the increased expression of HLA-I induced by S1P for both the percentages of cells and the MFI, upon comparing the effect of S1P to the effect of combining S1P with FTY720. [1] Medium and high-dose FTY720-P also enhances the levels of TGF-β1. TGF-β1 and Foxp3 mRNA expression are upregulated in the high-dose FTY720-P group. The proliferation of effector T cells is suppressed significantly in the medium and high-dose FTY720-P group at a Treg/Teff cell ratio of 1:1. At a ratio of 1:1, the proliferation of effector T cells is also suppressed in the high-dose FTY720 group. [2]
In vivo試験 FTY720 is effective in Ph+ but not Ph- ALL xenografts using an early disease model. FTY720 produces a significant reduction in disease burden in the Ph+ ALL xenografts using an early disease model. Ph+ human ALL xenografts responds to FTY720 with an 80 % reduction in overall disease if treatment has been initiated early on. In contrast, treatment of mice with FTY720 does not result in reduced leukemia compared to controls using four separate human Ph- ALL xenografts. [3]
臨床試験 FTY720 has enterd in a phase IV clinical trial in the treatment of multiple sclerosis anbd relapsing-remitting.
特集

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 Immature DCs
濃度 10 nM
反応時間 4 hours
実験の流れ Immature DCs are left intact or are incubated with 2 μM S1P, 10 nM FTY720, 10 nM SEW2871 or the combinations of S1P with these drugs for 4 hours. As a control 1 μg/mL LPS is used. The cells are washed and incubated in a 96-well plate (v-bottom, 2 × 105 cells per well), washed again and resuspended in PBS buffer containing 0.1% sodium azide. They are labeled with 1 μg/mL FITC-conjugated mouse anti-human CD80, 1 μg/mL FITC-conjugated mouse anti-human CD83, 1 μg/mL FITC-conjugated mouse anti-human CD86, 1 μg/mL FITC-conjugated mouse anti-human HLA-class I, 1 μg/mL FITC-conjugated mouse anti-human HLA-DR, 1 μg/mL FITC-conjugated mouse anti-human HLA-E, or 1 μg/mL FITC-conjugated mouse IgG as a control. The cells are washed twice, and examined in the flow cytometer. Markers are set according to the isotype control FITC-conjugated mouse IgG. To stain NK cells with antibodies for various NK cell activating receptors, they are either left untreated or incubated with 2 μM S1P for 4 hours, washed and stained with 1 μg/mL PE-conjugated mouse anti-human NKp30 (CD337), 1 μg/mL PE-conjugated mouse anti-human NKp44 (CD336), 1 μg/mL PE-conjugated mouse anti-human NKG2D (CD314), or as a control 1 μg/mL PE-conjugated mouse IgG1, for 45 min at 4 °C. NK cells are also stained with 1 μg/mL FITC-conjugated anti-killer inhibitory receptor (KIR)/CD158 antibody which recognizes KIR2DL2, KIR2DL3, KIR2DS2 and KIR2DS4, and as a control with FITC-conjugated mouse IgG. The cells are washed twice, and examined in the flow cytometer. Markers are set according to the isotype control PE-conjugated or FITC-conjugated mouse IgG.

動物実験: [3]

動物モデル NOD/SCIDγc−/− mice bearing ALL cells.
製剤 2% ethanol or saline
投薬量 5 mg/kg/day, 10 mg/kg/day
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Fingolimod (FTY720) HCl SDF
分子量 343.9
化学式

C19H33NO2.HCl

CAS No. 162359-56-0
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 69 mg/mL (200.63 mM)
69 mg/mL (200.63 mM)
エタノール 69 mg/mL (200.63 mM)
In vivo Saline 20 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 2-(4-octylphenethyl)-2-aminopropane-1,3-diol hydrochloride

カスタマーフィードバック (3)


Click to enlarge
Rating
Source Blood, 2012, 119, 2176-2177. Fingolimod (FTY720) HCl purchased from Selleck
Method Survival assay
Cell Lines SCID mice
Concentrations 2ug/g
Incubation Time 50 day
Results Fingolimod efficiently blocked rejection of both MOPC315 myeloma and F9 B-cell lymphoma by TCR-transgenic mice.

Click to enlarge
Rating
Source Blood, 2012, 119, 2176-2177. Fingolimod (FTY720) HCl purchased from Selleck
Method
Cell Lines SCID mice
Concentrations 1ug/g
Incubation Time 8 day
Results fingolimod blocks immunosurveillance of B-cell cancers by suppressing migration of tumor-specific Th1 cells from lymph nodes to the incipient tumor site, thereby preventing Th1-mediated activation of tumoricidal macrophages.

Click to enlarge
Rating
Source Mol Med, 2011, 17, 717- 725 . Fingolimod (FTY720) HCl purchased from Selleck
Method In vivo study
Cell Lines C57BL/6 WT animals
Concentrations 0.3 mg/kg
Incubation Time 9-15 day
Results Plasma sICAM-1, a marker of endothelialactivation (33), was decreased inFTY720-treated mice compared with untreatedmice (Figure 3A). Elevated levelsin infected but untreated mice were decreasedsignificantly in all animalstreated with FTY720 (P < 0.0001). Conversely,plasma Ang1, a marker of endotheliumquiescence and stability, wasincreased in mice treated with FTY720prophylactically compared with untreatedanimals (P = 0.02, Figure 3B).Studies observing Evans blue stainingof the brain demonstrated that FTY720treatment improved BBB integrity inECM.

文献中の引用 (23)

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related S1P受容体 モジュレータ

  • BAF312 (Siponimod)

    BAF312 (Siponimod) is a next-generation S1P receptor modulator, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively.

  • SB225002

    SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

  • Smoothened Agonist (SAG) HCl

    Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist.

  • SB-334867

    SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

  • PF-543

    PF-543 is a cell-permeant, selective sphingosine kinase 1 (Sphk1) inhibitor with Ki of 3.6 nM, >100-fold selective over SphK2.

    Features:The most potent inhibitor of SphK1 described to date.

  • SKI II

    SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2.

  • Vismodegib (GDC-0449)

    Vismodegib (GDC-0449)は、強力で、新しくて、特定のハリネズミ経路阻害剤で、 IC50 が 3 nMになる。

  • Forskolin

    Forskolin is a ubiquitous activator of eukaryotic adenylyl cyclase (AC), commonly used to raise levels of cAMP in the study and research of cell physiology.

  • Cyclopamine

    Cyclopamineは、スムーズにされる(SMO)ものの経路敵対者に合図している特定のハリネズミ(Hh)で、 IC50 が 46 nM。

最近チェックしたアイテム

Tags: Fingolimod (FTY720) HClを買う | Fingolimod (FTY720) HCl供給者 | Fingolimod (FTY720) HClを購入する | Fingolimod (FTY720) HCl費用 | Fingolimod (FTY720) HCl生産者 | オーダーFingolimod (FTY720) HCl | Fingolimod (FTY720) HCl代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ