E7766 diammonium salt

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。

E7766 diammonium salt  纯度: 99.73%

E7766 diammonium salt 是一种大环桥连 STING 激动剂,Kd 为 40 nM。E7766 diammonium salt 显示出强大的泛基因型和抗肿瘤活性。

E7766 diammonium salt

E7766 diammonium salt Chemical Structure

CAS No. : 2242635-03-4

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1 mg ¥5800 In-stock
5 mg ¥16500 In-stock
10 mg ¥26500 In-stock
50 mg   询价  
100 mg   询价  

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E7766 diammonium salt 相关产品

相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library

生物活性

E7766 diammonium salt is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 diammonium salt shows potent pan-genotypic and antitumor activities[1].

体外研究
(In Vitro)

E7766 diammonium salt inhibits four human STING variants, human wild-type, HAQ, AQ and REF STING proteins, with EC50 values of 1 μM, 2.2 μM, 1.2 μM and 4.9 μM, respectively[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)

In murine colon cancer model, a single intratumoral injection of 10 mg/kg E7766 diammonium salt in the subcutaneous tumor. E7766 diammonium salt is shown to have potent antitumor activity with long lasting immune memory response in a mouse liver metastatic tumor model[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.

Clinical Trial

分子量

780.66

Formula

C24H32F2N12O8P2S2

CAS 号

2242635-03-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

H2O : 45 mg/mL (57.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2810 mL 6.4048 mL 12.8097 mL
5 mM 0.2562 mL 1.2810 mL 2.5619 mL
10 mM 0.1281 mL 0.6405 mL 1.2810 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 and 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。

参考文献
  • [1]. Dae-Shik Kim, et al. E7766, a Macrocycle-Bridged Stimulator of Interferon Genes (STING) Agonist with Potent Pan-Genotypic Activity. ChemMedChem. 2021 Jun 7;16(11):1740-1743.

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PTP1B-IN-3 diammonium

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。

PTP1B-IN-3 diammonium 

PTP1B-IN-3 diammonium 是有效的,有选择性的 PTP1B 抑制剂,对 PTP1B 和 TCPTP 的 IC50 值均为 120 nM。PTP1B-IN-3 diammonium 具有抗糖尿病和抗癌作用。

PTP1B-IN-3 diammonium

PTP1B-IN-3 diammonium Chemical Structure

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1 mg ¥9500 In-stock
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生物活性

PTP1B-IN-3 diammonium is a potent and orally active PTP1B inhibitor with IC50s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 diammonium has antidiabetic and anticancer effects[1][2].

IC50 & Target

IC50: 120 nM (PTP1B), 120 nM (TCPTP)[2]

体内研究
(In Vivo)

In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits dose dependent inhibition (60%, 80% and 100% inhibition at 1, 3 and 10 mg/kg, respectively) of glucose excursion when given orally 2 h before oral glucose challenge with an estimated ED50 of 0.8 mg/kg[1].
In the NDL2 Ptpn1 transgenic mice, PTP1B-IN-3 (compounds 3g; orally; 30 mg/kg for 21 days) shows a significant delay in the onset of tumor development in NDL2 Ptpn1+/+ mice, extending the median tumor free days (T50) from 28 days to 75 days[1].
In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits good oral bioavailability (F of 24%), slow clearance (CL of 0.71 mL/kg/min), and good elimination half live (t1/2 of 6 h). The oral bioavailability in higher species such as rats (F of 4%) and squirrel monkeys (F of 2%) are substantially lower but excellent exposures are achieved with oral dosing[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

396.12

Formula

C12H13BrF2N3O3P

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

参考文献
  • [1]. Yongxin Han, et al. Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5.

    [2]. Price N, et al. Safety and Efficacy of a Topical Sodium Channel Inhibitor (TV-45070) in Patients With Postherpetic Neuralgia (PHN): A Randomized, Controlled, Proof-of-Concept, Crossover Study, With a Subgroup Analysis of the Nav1.7 R1150W Genotype. Clin J Pain. 2017 Apr;33(4):310-318.

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Cyclic-di-GMP diammonium(Synonyms: c-di-GMP diammonium; cyclic diguanylate diammonium; 5GP-5GP diammonium)

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。

Cyclic-di-GMP diammonium (Synonyms: c-di-GMP diammonium; cyclic diguanylate diammonium; 5GP-5GP diammonium) 纯度: ≥98.0%

Cyclic di-GMP (c-di-GMP) diammonium 是一种 STING 激活剂和无处不在的第二信使,调节生物膜的形成、运动和各种细菌的毒力。

Cyclic-di-GMP diammonium(Synonyms: c-di-GMP diammonium; cyclic diguanylate diammonium; 5GP-5GP diammonium)

Cyclic-di-GMP diammonium Chemical Structure

CAS No. : 609343-82-0

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1 mg ¥2500 In-stock
5 mg ¥7500 In-stock
10 mg   询价  
50 mg   询价  

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Cyclic-di-GMP diammonium 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

Cyclic di-GMP (c-di-GMP) diammonium is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species[1][2].

IC50 & Target[1][2]

Human Endogenous Metabolite

 

分子量

724.47

Formula

C20H30N12O14P2

CAS 号

609343-82-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 50 mg/mL (69.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3803 mL 6.9016 mL 13.8032 mL
5 mM 0.2761 mL 1.3803 mL 2.7606 mL
10 mM 0.1380 mL 0.6902 mL 1.3803 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。

参考文献
  • [1]. Wang Z, et al. STING activator c-di-GMP enhances the anti-tumor effects of peptide vaccines in melanoma-bearing mice. Cancer Immunol Immunother. 2015;64(8):1057-1066.

    [2]. Burdette DL, et al. STING is a direct innate immune sensor of cyclic di-GMP. Nature. 2011 Sep 25;478(7370):515-8.

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Diammonium Glycyrrhizinate(Synonyms: 甘草酸二铵)

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。

Diammonium Glycyrrhizinate (Synonyms: 甘草酸二铵) 纯度: 99.04%

Diammonium Glycyrrhizinate 可从甘草中分离得到,是一个广泛使用的抗炎化合物。

Diammonium Glycyrrhizinate(Synonyms: 甘草酸二铵)

Diammonium Glycyrrhizinate Chemical Structure

CAS No. : 79165-06-3

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10 mg ¥1400 In-stock
20 mg ¥2300 In-stock
50 mg   询价  
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  • FDA Approved & Pharmacopeial Drug Library

生物活性

Diammonium Glycyrrhizinate, isolated from the licorice root, is a widely used anti-inflammatory agent[1].

Clinical Trial

分子量

856.99

Formula

C42H68N2O16

CAS 号

79165-06-3

中文名称

甘草酸二铵

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (116.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1669 mL 5.8344 mL 11.6687 mL
5 mM 0.2334 mL 1.1669 mL 2.3337 mL
10 mM 0.1167 mL 0.5834 mL 1.1669 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 and 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: ≥ 2.5 mg/mL (2.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.92 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 (2.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.92 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 (2.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.92 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Yuan H, et al. Anti-inflammatory effect of Diammonium Glycyrrhizinate in a rat model of ulcerative colitis. World J Gastroenterol. 2006 Jul 28;12(28):4578-81.

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IACS-8803 diammonium

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。

IACS-8803 diammonium  纯度: 99.24%

IACS-8803 diammonium 是一种高效环状二核苷酸的 STING 激动剂,具有强大的全身抗肿瘤作用。

IACS-8803 diammonium

IACS-8803 diammonium Chemical Structure

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1 mg ¥5500 In-stock
5 mg ¥14500 In-stock
10 mg   询价  
50 mg   询价  

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IACS-8803 diammonium 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library

生物活性

IACS-8803 diammonium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 diammonium has a robust systemic antitumor efficacy[1].

体内研究
(In Vivo)

IACS-8803 diammonium (10 µg; intra-tumoral injection) shows superior antitumor activity in mice bearing bilateral B16-OVA melanomas[1].

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

分子量

726.60

Formula

C20H29FN12O9P2S2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

参考文献
  • [1]. Ager CR, et al. Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126640.

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