2. Immunology/Inflammation
  3. STING
  4. ZSA-215

ZSA-215 (2dr) (0-1.5 μM, 24 h) 在 THP1-Blue ISG 细胞中的 EC50 值低至 3.3 μM。
ZSA-215 (0.5-1.5μM, 24 h) 在THP1 细胞中对 STINGR232 (EC50 = 9.0 μM) 和 mSTING (EC50 = 9.3 μM) 表现出了最佳的活性。 ZSA-215 通过促进 STING、IRF3 的磷酸化以及 IFN-β 的分泌，增强了 STING 信号传导：
(1) ZSA-215 (6-13 μM, 24 h) 在THP1 细胞中显著增强了 IFN-β 的表达量。
(2) ZSA-215 (13-50μM, 3 h) 在 THP1-Blue ISG 细胞中显著增强了 STING 和 IRF3 的磷酸化水平。

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ZSA-215 Chemical Structure

ZSA-215 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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ZSA-215 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 inhibits tumor regression and long-term survival of mice in MC38 colon cancer model. ZSA-215 can be used to the study of colon cancerr[1].
体外研究
(In Vitro)

ZSA-215 (2dr) (0-1.5 μM, 24 h) 在 THP1-Blue ISG 细胞中的 EC50 值低至 3.3 μM[1]。

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

ZSA-215 相关抗体:

ELISA Assay[1]

Cell Line: THP1 cells
Concentration: 6 μM, 13 μM
Incubation Time: 24 h
Result: Enhanced STING signaling through promoting the secretion of IFN-β.

Western Blot Analysis[1]

Cell Line: THP1-Blue ISG cells
Concentration: 13 μM, 25 μM, 50 μM
Incubation Time: 3 h
Result: Significantly increased the phosphorylation of STING and IRF3.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 10 mg/kg p.o. T1/2 1.1 hr
Mice 5 mg/kg i.v. Cmax 48366.7 ng/mL
Mice 10 mg/kg p.o. Cmax 20633.3 ng/mL
Mice 5 mg/kg i.v. T1/2 0.6 hr
Mice 10 mg/kg p.o. CL 416.7 mL/h/kg
Mice 5 mg/kg i.v. AUC 20647.7 ng·h/mL
Mice 10 mg/kg p.o. AUC 23835 ng·h/mL
Mice 5 mg/kg i.v. CL 242.2 mL/h/kg
Mice 10 mg/kg p.o. F 58 %
体内研究
(In Vivo)

ZSA-215 (2dr) (60 mg/kg, PO, 每 3 天给药 1 次,共给药 2 or 6 剂) 在小鼠 MC38 肿瘤模型中显著抑制肿瘤生长，并且实现了长期存活[1]。

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

Animal Model: MC38 tumor model established in BALB/C female mice (6 weeks)[1]
Dosage: 60 mg/kg
Administration: PO, Every 3 Days, 2 or 6 doses
Result: Achieved CR and long-term survival of all mice, which significantly exceeded its parental compound ZSA-52 (CR = 60%) in combination with anti-PD-1.
Reached CR and long-term survival of all mice with monotherapy.
Did not show any tumor recurrence during additional 74 days observation (total 157 days observation).
Achieved a 60% complete response (CR) rate in mice following two-dose administration.
Produced a high concentration of IFN-β, IL-6 and CXCL10 in tumor and serum, which outperformed MSA-2.
分子量

402.28

Formula

C16H18FNO5Se
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ZSA-215 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

ZSA-215ZSA215ZSA 215STINGStimulator of Interferon GenesTMEM173MITAERISMPYSColon cancerIntramolecular hydrogen bond ring mimicMC38 colon cancer modelInhibitorinhibitorinhibit

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