1. GPCR/G Protein Immunology/Inflammation
  2. CXCR
  3. SCH 546738

SCH 546738 是一种有效、可口服的非竞争性 CXCR3 拮抗剂,结合到人 CXCR3 受体的亲和常数 (Ki) 为 0.4 nM。

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SCH 546738 Chemical Structure

SCH 546738 Chemical Structure

CAS No. : 906805-42-3

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     可免费申领三个不同产品的试用装。

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10 mg ¥3970
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Top Publications Citing Use of Products

    SCH 546738 purchased from MCE. Usage Cited in: Nat Commun. 2017 Nov 17;8(1):1571.  [Abstract]

    Activation of MAPK/ERK pathways after CXCR3 stimulation when cells are pretreated or not with CXCR3 antagonist SCH546738. Total ERK is used as loading control.

    SCH 546738 purchased from MCE. Usage Cited in: Theranostics. 2017 Sep 26;7(17):4192-4203.  [Abstract]

    Apoptosis related markers, ASK1, p-JNK, cleaved caspase 3 and cleaved PARP are measured by western blot in MCD-fed WT mice treated with vehicle or CXCR3 antagonists SCH546738 and AMG487.

    SCH 546738 purchased from MCE. Usage Cited in: J Hepatol. 2016 Jan;64(1):160-70.  [Abstract]

    CXCR3 antagonists suppress MCD-induced steatohepatitis in vivo. CXCR3 protein levels are decreased after 10 days treatment of CXCR3 antagonists.

    SCH 546738 purchased from MCE. Usage Cited in: J Allergy Clin Immunol. 2016 Jul;138(1):114-122.e4.  [Abstract]

    A selective CXCR3 receptor antagonist abrogates fibroblast migration to HRV MED (n=6).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.

    IC50 & Target[1]

    Human CXCR3

    0.4 nM (Ki)

    体外研究
    (In Vitro)

    SCH 546738 与人 CXCR3 受体结合的亲和力通过竞争结合分析确定,使用 35S 放射性标记的 SCH 535390 (CXCR3 化合物系列的磺胺类似物,Kd 为0.6 nM) 作为有竞争力的示踪剂。此外,SCH 546738 以非竞争性方式取代人类 CXCR3 中放射性标记的 CXCL10 和 CXCL11,IC50 范围为 0.8 至 2.2 nM。SCH 546738 在人活化的 T 细胞中有效且特异性地抑制 CXCR3 介导的趋化性,IC90 约为 10 nM[1]

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

    体内研究
    (In Vivo)

    SCH 546738 对猴、狗、小鼠和大鼠 [125I]hCXCL10 与 CXCR3 的结合具有较强的跨种活性,IC50 分别为 1.3、6.4、5.9 和 4.2 nM。SCH 546738 是一种选择性和有效的 CXCR3 拮抗剂,在体内研究中具有良好的PK [1]。

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

    分子量

    492.44

    Formula

    C23H31Cl2N7O

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 4.5 mg/mL (9.14 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 1 mg/mL (2.03 mM; 超声助溶 (<80°C))

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0307 mL 10.1535 mL 20.3070 mL
    5 mM 0.4061 mL 2.0307 mL 4.0614 mL
    查看完整储备液配制表

    * 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。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

    • 方案 一

      请依序添加每种溶剂: Corn Oil

      Solubility: 1 mg/mL (2.03 mM); 悬浊液; 超声加热助溶

    • 方案 二

      请依序添加每种溶剂: 0.5% Methylcellulose/saline water

      Solubility: 5 mg/mL (10.15 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献
    Cell Assay
    [1]

    The preparation of human activated T cells is performed. Human peripheral blood lymphocytes are prepared, depleted of monocytes, and stimulated for 2 days with 1 µg/mL PHA and 100 U/mL IL-2 in RPMI 1640 supplemented with 10% fetal bovine serum (FBS), 2 mM L-Glutamine, 1% non-essential amino acids and 2 mM HEPES. Following stimulation, peripheral blood lymphocytes are cultured in above media containing 5% conditioned media for up to 15 days. uman activated T cell chemotaxis assays ae performed using 96-well ChemoTx microplates with a 3 µm filter. Activated T cells are washed with RPMI medium twice, and then resuspended in the medium containing 20% FBS. 1.25×105 cells/reaction are mixed with indicated concentrations of SCH 546738 (1, 10 or 100 nM) and placed on the filter. SCH 546738 and chemokines are mixed and placed in the bottom well of the ChemoTx system. After 2.5 hours incubation at 37°C/5% CO2, the cells are scraped off and the plate system is centrifuged for 5 minutes at 1000 RPM. The filter screen is then removed and the ChemoTx plate is inverted into a 96 well plate with a funnel plate. The plate system is centrifuged for 5 minutes at 1000 RPM. The volume in the wells is brought to 100 μL with assay buffer and the plates are rested for approximately 15 minutes at room temperature. The number of migrated cells is measured using the Cell Titer Glo Luminescent Assay. Chemotaxis is expressed as a chemotactic index, which is a ratio versus the one without chemokines[1]

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

    Animal Administration
    [1]

    Mice[1]
    Female C57BL/6 mice are used. For immunization, 150 μg MOG35-55 peptide prepared by Princeton Biomolecules and 300 μg killed Mycobacterium tuberculosis are mixed in CFA and injected s.c. in two 50-μL injections over the flanks on day 1. Also, 200 ng of pertussis toxin is injected i.v. on days 0 and 2. SCH 546738 is administered orally 30 mpk in C57BL/6 mice twice daily. Dosing with SCH 546738 started at day 0, 24 h prior to MOG35-55 immunization (day 1). Mice are monitored daily and assessed for clinical signs of disease in a blinded fashion according to the following criteria: 0, no signs of disease; 1, tail paralysis; 2, limp tail and hind limb weakness; 3, hind limb paralysis; 4, hind limb plus forelimb paralysis; and 5, moribund or dead. Cumulative clinical scores are calculated by adding daily scores from the day of immunization until the end of the experiment. Mean clinical scores at separate days and mean maximal scores are calculated by adding the scores of individual mice and dividing with the number of mice in each group, including mice not developing signs of EAE.
    Rats[1]
    Male Lewis rats challenged by injection of 50 µL (30 mg) of a guinea pig spinal cord homogenate in complete Freund's adjuvant (CFA) into one footpad. SCH 546738 or 0.4% methylcellulose (vehicle) is orally administered at the indicated dose (0.2 mL) twice a day, starting on the day before transplantation until the day of graft rejection. SCH 546738 is administered orally at 10 mg/kg (mpk) in Lewis rats. To test whether SCH 546738 enhances the effect of conventional immunosuppressive reagent, the recipients are received treatment with subtherapeutic dose of CsA for one week combined with treatment with SCH 546738. Graft survival is analyzed using the log-rank test. The parametric data are analyzed by Student t test (2-tailed) using GraphPad InStat version.

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

    参考文献

    SCH 546738 相关分类

    完整储备液配制表

    * 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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.0307 mL 10.1535 mL 20.3070 mL 50.7676 mL
    DMSO 5 mM 0.4061 mL 2.0307 mL 4.0614 mL 10.1535 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
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    目录号:
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