1. Immunology/Inflammation
  2. SPHK
  3. Opaganib

Opaganib (Synonyms: ABC294640)

目录号: HY-16015 纯度: 99.68%
产品使用指南

Opaganib (ABC294640) 是一种选择性的竞争性的鞘氨醇激酶 2 (SK2) 抑制剂,Ki 为 9.8 μM。

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Opaganib Chemical Structure

Opaganib Chemical Structure

CAS No. : 915385-81-8

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥1045 In-stock
5 mg ¥950 In-stock
10 mg ¥1500 In-stock
50 mg ¥5000 In-stock
100 mg ¥7900 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Top Publications Citing Use of Products

    Opaganib purchased from MCE. Usage Cited in: Oncotarget. 2016 Mar 29;7(13):16663-75.

    The western blot demonstrates the effect of ABC294640 (25 μM) for 24 h in the presence and absence of MG132 (10 μM) on Des1 expression. Actin is used a protein loading control.

    Opaganib purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836.

    NRK-49F cells are treated with TGF-β1 for the indicated time. The levels of p-STAT3, p-AKT, p-GSK3α, and p-GSK3β expression are detected in comparison with the levels of total STAT3, AKT, GSK3α, GSK3β, and with GAPDH as the loading control.

    Opaganib purchased from MCE. Usage Cited in: Arch Med Res. 2018 Jul;49(5):335-341.

    Inhibition of SphK2 by si-RNA (si-SphK2) and ABC294640 (ABC) decrease phosphorylation and acetylation of STAT3 . Also, both si-RNA and ABC294640 reverse IL-6 induced increasing phosphorylation and acetylation of STAT3.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    Description

    Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.

    IC50 & Target

    Ki: 9.8 μM (SK2)[1]

    In Vitro

    Using recombinant human SK1 and SK2, Opaganib demonstrates dose-dependent inhibition of SK2 with an IC50 of approximately 60 μM without affecting the activity of SK1 at concentrations up to at least 100 μM. In contrast, N,N-dimethylsphingosine (DMS) inhibits both SK1 and SK2 with IC50 values of approximately 60 and 20 μM, respectively. Kinetic analyses of varying concentrations of Opaganib (ABC294640) in the presence of 2.5 to 25 μM sphingosine indicated a Ki of 9.8±1.4 μM for the inhibition of SK2. Opaganib (ABC294640) decreases [3H]S1P formation in a dose-dependent fashion with an IC50 value of 26 μM[1]. IC50 values for Opaganib (ABC294640) are approximately 50 and 60 μM for A-498 and Bxpc-3 cells, respectively; whereas the IC50 values for Opaganib (ABC294640) are approximately 20 and 40 μM for these cells[2].

    In Vivo

    Opaganib induces a transient minor decrease in the hematocrit of rats. Hematology studies indicate decreases in red blood cell number and hematocrit of approximately 20% in animals given either 100 or 250 mg/kg/day; and a slight increase in neutrophils and decrease in basophils in the treated rats[1]. Mice are gavaged with Opaganib (50 mg/kg), a selective inhibitor of sphingosine kinase-2 (SK2), 1 h before surgery and subjected to 1 h-warm ischemia to ~70% of the liver followed by reperfusion. Opaganib-treatment largely prevented the increase of sphingosine-1-phosphate (S1P) after ischemia-reperfusion (IR) in vivo[2].

    Clinical Trial
    Molecular Weight

    380.91

    Formula

    C₂₃H₂₅ClN₂O

    CAS No.

    915385-81-8

    SMILES

    O=C(C1(C2)CC3(C4=CC=C(Cl)C=C4)CC2CC(C3)C1)NCC5=CC=NC=C5

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (262.53 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6253 mL 13.1265 mL 26.2529 mL
    5 mM 0.5251 mL 2.6253 mL 5.2506 mL
    10 mM 0.2625 mL 1.3126 mL 2.6253 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.56 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.56 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.56 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    References
    Cell Assay
    [1]

    To determine the effects of the test compounds (e.g., Opaganib (ABC294640)) on proliferation, cells are plated into 96-well microtiter plates and allowed to attach for 24 h. Varying concentrations of Opaganib are added to individual wells and the cells are incubated for an additional 72 h. At the end of this period, the number of viable cells is determined by use of the sulforhodamine-binding assay. The percentage of cells killed is calculated as the percentage decrease in sulforhodamine-binding compare with control cultures. Regression analyses of inhibition curves are performed by use of GraphPad Prism[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][3]

    Rats[1]
    Sprague-Dawley male rats (7-8 weeks old) are orally dosed with 0, 100, or 250 mg of ABC294640•HCl/kg in 0.375% Polysorbate-80 in PBS daily for 7 days. The animals are observed daily for viability, signs of gross toxicity, and behavioral changes, and a battery of detailed observations are performed on study days 1 and 7. Blood is sampled from all animals on day 8 of the study for hematology, clinical biochemistry, and serology assessments, and the animals are sacrificed. Gross necropsies are performed on all study rats, and selected organs and tissues are evaluated in the control and high-dose level groups.
    Mice[3]
    Male C57BL/6 (8-9 weeks) mice are gavaged with 50 mg/kg of Opaganib (ABC294640), or an equivalent volume of vehicle (0.375% Tween 80 in phosphate buffered saline, pH 7.1) 1 h before surgery. Under ether anesthesia, ischemia to 70% of the total liver is induced for 1 h. After opening the vascular clamp, the non-ischemic liver lobes are removed, and mice are observed 7 days for survival. Sham operation included equivalent anesthesia and laparotomy without ischemia.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.68%

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    Keywords:

    OpaganibABC294640ABC 294640ABC-294640SPHKSphingosine kinaseInhibitorinhibitorinhibit

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    产品名称:
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    目录号:
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