标签归档：sting

STING agonist-7

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

STING agonist-7 

STING agonist-7 是一种非核苷酸 STING 激动剂，选择性结合小鼠 STING 而不是人类 STING。STING agonist-7 穿透细胞膜较差。

STING agonist-7

STING agonist-7 Chemical Structure

规格 是否有货
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生物活性

STING agonist-7 is a non-nucleotide STING agonist. STING agonist-7 binds selectively to mouse STING but not human STING. STING agonist-7 penetrates cell membrane poorly[1].

体外研究
(In Vitro)

STING agonist-7 (compound 11) is active in biochemical assays but inactive in cellular reporter assays[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

336.30

Formula

C17H12N4O4
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.
参考文献

  • [1]. Emily C Cherney, et al. Discovery of Non-Nucleotide Small-Molecule STING Agonists via Chemotype Hybridization. J Med Chem. 2022 Feb 24;65(4):3518-3538.

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MSA-2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MSA-2  纯度: 98.79%

MSA-2 是一种口服非核苷酸 STING 激动剂，以具有纳摩尔亲和力的非共价二聚体形式与 STING 结合。MSA-2 对人的 STING 亚型 WT 和 HAQ 的 EC50 分别为 8.3 和 24 μM。MSA-2 在同基因小鼠肿瘤模型中显示抗肿瘤活性，刺激肿瘤分泌干扰素-β，诱导肿瘤消退，具有持久的抗肿瘤免疫，并与抗 PD-1 协同作用。

MSA-2

MSA-2 Chemical Structure

CAS No. : 129425-81-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥3100 In-stock
10 mg ￥5200 In-stock
25 mg ￥9800 In-stock
50 mg ￥15000 In-stock
100 mg ￥22000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MSA-2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Orally Active Compound Library

生物活性

MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models[1][2].

体内研究
(In Vivo)

MSA-2 dosed via either PO or SC regimens achieved comparable exposure in both tumor and plasma. MSA-2 also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes, and dosing regimens were identified that induced complete tumor regressions in 80 to 100% of treated animals[1].
MSA-2 (PO: 60 mg/kg or SC: 50 mg/kg; single dose) that effectively inhibits tumor growth induced substantial elevations of IFN-β, interleukin-6 (IL-6), and TNF-α in tumor[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MC38 tumor-bearing C57BL6 mice[1]
Dosage: 60 mg/kg
Administration: P.o. ; s.c (50 mg/kg); single dose
Result: PO or SC doses of MSA-2 that effectively inhibited tumor growth induced substantial elevations of IFN-β, interleukin-6 (IL-6), and TNF-α in tumor.

分子量

294.32

Formula

C14H14O5S
CAS 号

129425-81-6
运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (169.88 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3977 mL 16.9883 mL 33.9766 mL
5 mM 0.6795 mL 3.3977 mL 6.7953 mL
10 mM 0.3398 mL 1.6988 mL 3.3977 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 (protect from light)。-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: ≥ 2.08 mg/mL (7.07 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.07 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (7.07 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.07 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Pan BS, et al. An orally available non-nucleotide STING agonist with antitumor activity. Science. 2020;369(6506):eaba6098.

    [2]. Liu J, et al. Identification of MSA-2: An oral antitumor non-nucleotide STING agonist. Signal Transduct Target Ther. 2021;6(1):18. Published 2021 Jan 12.

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diABZI STING agonist-1 trihydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

diABZI STING agonist-1 trihydrochloride  纯度: 99.92%

diABZI STING agonist-1 (trihydrochloride) 是一个选择性的干扰素基因刺激受体 (STING) 的激动剂，其在人和小鼠中的 EC50 值分分别为 130 nM 和 186 nM。

diABZI STING agonist-1 trihydrochloride

diABZI STING agonist-1 trihydrochloride Chemical Structure

CAS No. : 2138299-34-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥6300 In-stock
5 mg ￥3500 In-stock
10 mg ￥5900 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

diABZI STING agonist-1 trihydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library

生物活性

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

IC50 & Target

STING[1].
体外研究
(In Vitro)

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

diABZI STING agonist-1 trihydrochloride (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo[1].
diABZI STING agonist-1 trihydrochloride (intravenous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (200 ng/ml)[1].
diABZI STING agonist-1 trihydrochloride (intravenous injection; 1.5 mg/kg; days 1, 4 and 8; 43 days) results in significant tumour growth inhibition and significantly improves survival (P < 0.001) with 8 out of 10 mice remaining tumor free at the end of the study on day 43[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wild and Sting−/− C57Blk6 mice[1]
Dosage: 2.5 mg/kg
Administration: Subcutaneous injection; 2.5 mg/kg
Result: Activated secretion of IFNβ, IL-6, TNF, and CXCL1 in wild-type but not Sting−/− mice.
Animal Model: Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice[1]
Dosage: 3 mg/kg
Administration: Intravenous injection; 3 mg/kg
Result: Exhibited a half-life of 1.4 hours and achieved systemic concentrations greater than EC50 for mouse STING (200 ng/ml).
Animal Model: Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice[1]
Dosage: 1.5 mg/kg
Administration: Intravenous injection; 1.5 mg/kg; 43 days
Result: Resulted in significant tumour growth inhibition and improved survival.

分子量

959.32

Formula

C42H54Cl3N13O7
CAS 号

2138299-34-8
运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : 100 mg/mL (104.24 mM; Need ultrasonic)

DMSO : 90 mg/mL (93.82 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0424 mL 5.2120 mL 10.4241 mL
5 mM 0.2085 mL 1.0424 mL 2.0848 mL
10 mM 0.1042 mL 0.5212 mL 1.0424 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 (sealed storage, away from moisture)。-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: ≥ 2.08 mg/mL (2.17 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.17 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (2.17 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.17 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (2.17 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.17 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 20.8 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7.

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STING agonist-3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

STING agonist-3  纯度: 99.96%

STING agonist-3 源于专利 WO2017175147A1 (实施例10)，是一种选择性和非核苷酸的小分子 STING 激动剂，pEC50 和 pIC50 分别为 7.5 和 9.5。STING agonist-3 具有持久的抗肿瘤作用，并且在改善癌症研究方面具有巨大潜力。

STING agonist-3

STING agonist-3 Chemical Structure

CAS No. : 2138299-29-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5780 In-stock
5 mg ￥4000 In-stock
10 mg ￥7000 In-stock
25 mg ￥11000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

STING agonist-3 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library

生物活性

STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer[1].

体外研究
(In Vitro)

STING agonist-3 exhibits a pEC50 value of 7.5 in activation of STING in cells, this assay is determined using a luciferase reporter assay in human embryonic kidney cells (HEK293T) co-transfected with plasmids expressing STING and the enzyme firefly luciferase driven by the interferon stimulated response element promoter[1].
STING agonist-3 exhibits a pIC50 value of 9.5 in FRET assay. This is a competition binding assay which aims to determine the binding potency of molecules to the C-terminal Domain (CTD) of human STING[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

750.81

Formula

C37H42N12O6
CAS 号

2138299-29-1
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 : 41.67 mg/mL (55.50 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3319 mL 6.6595 mL 13.3189 mL
5 mM 0.2664 mL 1.3319 mL 2.6638 mL
10 mM 0.1332 mL 0.6659 mL 1.3319 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: ≥ 2.08 mg/mL (2.77 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.77 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: 2.08 mg/mL (2.77 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (2.77 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (2.77 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.77 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 20.8 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Adam Kenneth, et al. Heterocyclic amides useful as protein modulators.patent WO2017175147A1

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

STING agonist-3 trihydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

STING agonist-3 trihydrochloride 

STING agonist-3 trihydrochloride 源于专利 WO2017175147A1 (实施例10)，是一种选择性和非核苷酸的小分子 STING 激动剂，pEC50 和 pIC50 分别为 7.5 和 9.5。STING agonist-3 trihydrochloride 具有持久的抗肿瘤作用，并且在改善癌症研究方面具有巨大潜力。

STING agonist-3 trihydrochloride

STING agonist-3 trihydrochloride Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

STING agonist-3 trihydrochloride 的其他形式现货产品:

STING agonist-3

生物活性

STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pEC50 of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer[1].

IC50 & Target

STING[1]
体外研究
(In Vitro)

STING agonist-3 trihydrochloride exhibits a pEC50 value of 7.5 in activation of STING in cells, this assay is determined using a luciferase reporter assay in human embryonic kidney cells (HEK293T) co-transfected with plasmids expressing STING and the enzyme firefly luciferase driven by the interferon stimulated response element promoter[1].
STING agonist-3 trihydrochloride exhibits a pIC50 value of 9.5 in FRET assay. This is a competition binding assay which aims to determine the binding potency of molecules to the C-terminal Domain (CTD) of human STING[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

860.19

Formula

C37H45Cl3N12O6
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.
参考文献

  • [1]. Adam Kenneth, et al. Heterocyclic amides useful as protein modulators.patent WO2017175147A1

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STING agonist-4

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

STING agonist-4  纯度: 98.08%

STING agonist-4 是干扰素基因 (STING) 的受体激动剂的刺激剂，它的表观抑制常数 IC50 为 20 nM，STING agonist-4 是一种含两个对称相关的氨基苯并咪唑 (ABZI) 基的化合物。

STING agonist-4

STING agonist-4 Chemical Structure

CAS No. : 2138300-40-8

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10 mg ￥5000 In-stock
50 mg ￥15000 In-stock
100 mg ￥21000 In-stock
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STING agonist-4 相关产品

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  • Bioactive Compound Library Plus

生物活性

STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function[1].

IC50 & Target

IC50: 20 nM (STING agonist-4)[1]
体外研究
(In Vitro)

STING agonist-4 (Compound 2) (0.3-30 μM; 2 hours) causes phosphorylation of IRF3 and STING that is inhibited by the TBK1 inhibitor BX795 and induces dose-dependent secretion of IFN-β with an EC50 of 3.1 μM[1].
STING agonist-4 (Compound 2) (0.001 nM-1 μM) inhibits binding of full-length STING to the solid support with an apparent dissociation constant (Kd) of approximately 1.6 nM[1].
STING agonist-4 (Compound 2) (0-100 μM) is 18-fold more potent than cGAMP (an endogenous STING ligand), with an EC50 of 53.9 μM[1].
STING agonist-4 (Compound 2) (3 μM; 4 hours) promotes production of interferon γ-induced protein 10 (IP-10), IL-6 and TNF-α by a mechanism that is dependent on STING-mediated activation of TBK1[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Human peripheral blood mononuclear cells (PBMCs)
Concentration: 0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM
Incubation Time: 2 hours
Result: Caused phosphorylation of IRF3 and STING and induced secretion of IFN-β.

分子量

678.74

Formula

C34H38N12O4
CAS 号

2138300-40-8
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 : 10 mg/mL (14.73 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

*STING agonist-4 is usually formulated as a suspension.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4733 mL 7.3666 mL 14.7332 mL
5 mM 0.2947 mL 1.4733 mL 2.9466 mL
10 mM 0.1473 mL 0.7367 mL 1.4733 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: 1 mg/mL (1.47 mM); Suspended solution; Need ultrasonic

    此方案可获得 1 mg/mL (1.47 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 10.0 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: 1 mg/mL (1.47 mM); Suspended solution; Need ultrasonic

    此方案可获得 1 mg/mL (1.47 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 10.0 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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Ramanjulu JM et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Dec;564(7736):439-443.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务