标签归档：pde

EHNA hydrochloride(Synonyms: 外消旋-9-(2-羟基-3-壬基)腺嘌呤盐酸盐)

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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。

EHNA hydrochloride (Synonyms: 外消旋-9-(2-羟基-3-壬基)腺嘌呤盐酸盐) 纯度: 99.61%

EHNA hydrochloride 是一个强有力的和选择性的环核苷酸磷酸二酯酶 2 (PDE2) (IC50=4 μM) 和腺苷脱氨酶 (ADA) 的双重抑制剂。EHNA hydrochloride 浓度依耐性抑制 cGMP 刺激的 PDE2 的活性，IC50 值分别为 0.8 μM (人类) 和 2 μM (猪心肌)，但是对没有刺激的 PDE2 抑制力较小。EHNA hydrochloride 在调节多种药理反应中发挥作用，包括抗病毒、抗肿瘤和抗心律失常作用。

EHNA hydrochloride(Synonyms: 外消旋-9-(2-羟基-3-壬基)腺嘌呤盐酸盐)

EHNA hydrochloride Chemical Structure

CAS No. : 58337-38-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2762 In-stock
2 mg ￥1600 In-stock
5 mg ￥2500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

EHNA hydrochloride 相关产品

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  • Antiviral Compound Library
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  • Anti-Alzheimer’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects[1][2].

IC50 & Target[1]

hPDE2A

0.8 μM (IC50)

体外研究
(In Vitro)

EHNA completely ablates the ability of cyclic GMP to activate PDE2 activity, whilst having a much smaller inhibitory effect on the unstimulated PDE2 activity[2].
EHNA exhibits normal Michaelian kinetics of inhibition for the cyclic GMP-stimulated PDE2 activity with Hill plots near unity[2].
EHNA prevents dAdo degradation and increases mitochondrial dATP levels in fibroblasts[3].

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

313.83

Formula

C14H24ClN5O
CAS 号

58337-38-5
中文名称

外消旋-9-(2-羟基-3-壬基)腺嘌呤盐酸盐
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: 

DMSO : ≥ 250 mg/mL (796.61 mM)

H2O : 100 mg/mL (318.64 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1864 mL 15.9322 mL 31.8644 mL
5 mM 0.6373 mL 3.1864 mL 6.3729 mL
10 mM 0.3186 mL 1.5932 mL 3.1864 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 (6.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.63 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 (6.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.63 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 (6.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.63 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]. Podzuweit T, et al. Isozyme selective inhibition of cGMP-stimulated cyclic nucleotide phosphodiesterases by erythro-9-(2-hydroxy-3-nonyl) adenine.Cell Signal. 1995 Sep;7(7):733-8.

    [2]. Michie AM, et al. Rapid regulation of PDE-2 and PDE-4 cyclic AMP phosphodiesterase activity following ligation of the T cell antigen receptor on thymocytes: analysis using the selective inhibitors erythro-9-(2-hydroxy-3-nonyl)-adenine (EHNA) and rolipram.Cell Signal. 1996 Feb;8(2):97-110.

    [3]. Blázquez-Bermejo C, et al. Increased dNTP pools rescue mtDNA depletion in human POLG-deficient fibroblasts. FASEB J. 2019 Jun;33(6):7168-7179.

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PDE4-IN-8

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。

PDE4-IN-8 

PDE4-IN-8 (Example 5) 是一种有效的 PDE4 抑制剂，对 PDE4B2 的 IC50为 0.93 nM。PDE4-IN-8 对 IL13、IL4、IFNy 的有微弱的抑制作用，IC50 分别为 4.04 nM, 36.33 nM, 2394 nM。

PDE4-IN-8

PDE4-IN-8 Chemical Structure

CAS No. : 2415085-45-7

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

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生物活性

PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC50 of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC50=4.04 nM), IL4 (IC50=36.33 nM), IFNy (IC50=2394 nM)[1].

IC50 & Target[1]

PDE4B2

0.93 nM (IC50)

IL4

36.33 nM (IC50)

IL-13

4.04 nM (IC50)

分子量

327.18

Formula

C18H22BNO4
CAS 号

2415085-45-7
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]. Joseph Walter Strohbach, et al. Inhibiteurs de pde4 contenant du bore. WO2020070651A1.

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

PDE4-IN-8

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。

PDE4-IN-8 

PDE4-IN-8 (Example 5) 是一种有效的 PDE4 抑制剂，对 PDE4B2 的 IC50为 0.93 nM。PDE4-IN-8 对 IL13、IL4、IFNy 的有微弱的抑制作用，IC50 分别为 4.04 nM, 36.33 nM, 2394 nM。

PDE4-IN-8

PDE4-IN-8 Chemical Structure

CAS No. : 2415085-45-7

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

* Please select Quantity before adding items.

生物活性

PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC50 of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC50=4.04 nM), IL4 (IC50=36.33 nM), IFNy (IC50=2394 nM)[1].

IC50 & Target[1]

PDE4B2

0.93 nM (IC50)

IL4

36.33 nM (IC50)

IL-13

4.04 nM (IC50)

分子量

327.18

Formula

C18H22BNO4
CAS 号

2415085-45-7
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]. Joseph Walter Strohbach, et al. Inhibiteurs de pde4 contenant du bore. WO2020070651A1.

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

PDE4-IN-8

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。

PDE4-IN-8 

PDE4-IN-8 (Example 5) 是一种有效的 PDE4 抑制剂，对 PDE4B2 的 IC50为 0.93 nM。PDE4-IN-8 对 IL13、IL4、IFNy 的有微弱的抑制作用，IC50 分别为 4.04 nM, 36.33 nM, 2394 nM。

PDE4-IN-8

PDE4-IN-8 Chemical Structure

CAS No. : 2415085-45-7

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

* Please select Quantity before adding items.

生物活性

PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC50 of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC50=4.04 nM), IL4 (IC50=36.33 nM), IFNy (IC50=2394 nM)[1].

IC50 & Target[1]

PDE4B2

0.93 nM (IC50)

IL4

36.33 nM (IC50)

IL-13

4.04 nM (IC50)

分子量

327.18

Formula

C18H22BNO4
CAS 号

2415085-45-7
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]. Joseph Walter Strohbach, et al. Inhibiteurs de pde4 contenant du bore. WO2020070651A1.

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

Deltarasin

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。

Deltarasin  纯度: 99.89%

Deltarasin 是一种 KRAS-PDEδ 相互作用的抑制剂，能够与 PDEδ 结合，Kd 值为 38 nM。

Deltarasin

Deltarasin Chemical Structure

CAS No. : 1440898-61-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2223 In-stock
2 mg ￥1116 In-stock
5 mg ￥1674 In-stock
10 mg ￥2511 In-stock
50 mg ￥8277 In-stock
100 mg ￥13020 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Deltarasin 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Ferroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Deltarasin is an inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

IC50 & Target

Kd: 38 nM (PDEδ)
体外研究
(In Vitro)

In liver cells, deltarasin inhibits the interaction of RAS with PDEδ with Kd of 41 nM. Inhibition of PDEδ-KRAS interaction by deltarasin suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS[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)

Deltarasin (10 mg/kg, i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumour cell xenografts[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

603.75

Formula

C40H37N5O
CAS 号

1440898-61-2
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 : ≥ 42 mg/mL (69.57 mM)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6563 mL 8.2816 mL 16.5631 mL
5 mM 0.3313 mL 1.6563 mL 3.3126 mL
10 mM 0.1656 mL 0.8282 mL 1.6563 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:
  • 1.

    Deltarasin is prepared in PBS[2].
参考文献

  • [1]. Zimmermann G, et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013 May 30;497(7451):638-42.

    [2]. Agalioti T, et al. Mutant KRAS promotes malignant pleural effusion formation. Nat Commun. 2017 May 16;8:15205. doi: 10.1038/ncomms15205.
Kinase Assay
[1]

Kd values are measured by fluorescence polarization measurements. For direct titrations, increasing amounts of PDEδ are added to a solution containing 50-100 nM labelled small molecule in 200 µL PBS buffer. For displacement titrations, increasing amounts of the small molecules in DMSO are directly added to fluorescein-labelled atorvastatin (24 nM) and His6-tagged PDEδ (40 nM) in 200 µL PBS-buffer (containing 0.05% CHAPS, 1% DMSO), keeping the concentration of fluorescein-labelled atorvastatin, PDEδ and DMSO constant. For Kd measurements using isothermal titration calorimetry, PDEδ protein (280 µM) is titrated to small molecule (30 µM) in Tris/HCl buffer (temperature 25°C). In the Tm shift assays, protein melting points are detected by circular dichroism spectroscopy in the presence of small molecules.

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.
参考文献

  • [1]. Zimmermann G, et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013 May 30;497(7451):638-42.

    [2]. Agalioti T, et al. Mutant KRAS promotes malignant pleural effusion formation. Nat Commun. 2017 May 16;8:15205. doi: 10.1038/ncomms15205.

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Deltarasin hydrochloride

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。

Deltarasin hydrochloride  纯度: 99.97%

Deltarasin hydrochloride 能抑制 KRAS 与 PDEδ 相互作用，与 PDEδ 结合的 Kd 为 41 nM。

Deltarasin hydrochloride

Deltarasin hydrochloride Chemical Structure

CAS No. : 1613404-76-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2358 In-stock
2 mg ￥1116 In-stock
5 mg ￥1674 In-stock
10 mg ￥2511 In-stock
50 mg ￥8277 In-stock
100 mg ￥13020 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with Kd of 38 nM for binding to purified PDEδ.

IC50 & Target

Kd: 38 nM (PDEδ)
体外研究
(In Vitro)

In liver cells, deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Inhibition of PDEδ-KRAS interaction by deltarasin suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Deltarasin (10 mg/kg, i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumour cell xenografts[1].

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

640.22

Formula

C40H38ClN5O
CAS 号

1613404-76-4
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: 

DMSO : ≥ 52 mg/mL (81.22 mM)

H2O : 50 mg/mL (78.10 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5620 mL 7.8098 mL 15.6196 mL
5 mM 0.3124 mL 1.5620 mL 3.1239 mL
10 mM 0.1562 mL 0.7810 mL 1.5620 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]. Zimmermann G, et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013 May 30;497(7451):638-42.
Kinase Assay
[1]

KD values are measured by fluorescence polarization measurements. For direct titrations, increasing amounts of PDEδ are added to a solution containing 50-100 nM labelled small molecule in 200 µL PBS buffer. For displacement titrations, increasing amounts of the small molecules in DMSO are directly added to fluorescein-labelled atorvastatin (24 nM) and His6-tagged PDEδ (40 nM) in 200 µL PBS-buffer (containing 0.05% CHAPS, 1% DMSO), keeping the concentration of fluorescein-labelled atorvastatin, PDEδ and DMSO constant. For KD measurements using isothermal titration calorimetry, PDEδ protein (280 µM) is titrated to small molecule (30 µM) in Tris/HCl buffer (temperature 25°C). In the Tm shift assays, protein melting points are detected by circular dichroism spectroscopy in the presence of small molecules.

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

  • [1]. Zimmermann G, et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013 May 30;497(7451):638-42.

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