标签归档：diabzi

diABZI-C2-NH2

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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-C2-NH2  纯度: 96.02%

diABZI-C2-NH2是一种含有伯胺功能的活性类似物，是一种 STING 激动剂。

diABZI-C2-NH2

diABZI-C2-NH2 Chemical Structure

CAS No. : 2137975-93-8

规格 价格 是否有货 数量
5 mg ￥7800 In-stock
10 mg ￥12500 In-stock
50 mg   询价  
100 mg   询价  

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diABZI-C2-NH2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

diABZI-C2-NH2, an active analogue containing a primary amine functionality, is a STING agonist[1].

体外研究
(In Vitro)

The author developed a linking strategy to synergize the effect of two symmetry-related amidobenzimidazole (ABZI)-based compounds to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function. Intravenous administration of a diABZI STING agonist to immunocompetent mice with established syngeneic colon tumours elicited strong anti-tumour activity, with complete and lasting regression of tumors[1].
diABZI-C2-NH2 is covalently immobilized on sepharose beads and is used to affinity-capture potential target proteins from a THP1 cell lysate[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

721.81

Formula

C36H43N13O4
CAS 号

2137975-93-8
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
参考文献

  • [1]. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity [published correction appears in Nature. 2019 Jun;570(7761):E53]. Nature. 2018;564(7736):439-443.

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diABZI STING agonist-1 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。

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.

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