标签归档：ibudilast

Ibudilast-d3 (Synonyms: 异丁司特 d3)

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。

Ibudilast-d3  (Synonyms: 异丁司特 d3)

Ibudilast-d3 是 Ibudilast 的氘代物。Ibudilast (KC-404; AV-411; MN-166) 是一种环腺苷酸磷酸二酯酶 (PDE) 抑制剂。Ibudilast 具有抗血小板聚集作用。Ibudilast 抑制气管平滑肌收缩性，可用于哮喘的研究。Ibudilast 可能是一种有效的神经保护和抗痴呆药物，可对抗活化小胶质细胞的神经毒性。

Ibudilast-d3 (Synonyms: 异丁司特 d3)

Ibudilast-d3 Chemical Structure

CAS No. : 102064-45-9

规格 是否有货
1 mg Check price and availability
10 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Ibudilast-d3 (KC-404-d3) is the deuterium labeled Ibudilast. Ibudilast (KC-404) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

233.32

Formula

C14H14D4N2O
CAS 号

102064-45-9
中文名称

异丁司特 d3
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Mizuno T, et al. Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia. Neuropharmacology. 2004 Mar;46(3):404-11.

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

生物活性分子抑制剂Ibudilast(Synonyms: 异丁司特; KC-404; AV-411; MN-166)

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。

Ibudilast (Synonyms: 异丁司特; KC-404; AV-411; MN-166) 纯度: 99.89%

Ibudilast (KC-404; AV-411; MN-166) 是一种环腺苷酸磷酸二酯酶 (PDE) 抑制剂。Ibudilast 具有抗血小板聚集作用。Ibudilast 抑制气管平滑肌收缩性，可用于哮喘的研究。Ibudilast 可能是一种有效的神经保护和抗痴呆药物，可对抗活化小胶质细胞的神经毒性。

Ibudilast(Synonyms: 异丁司特; KC-404; AV-411; MN-166)

Ibudilast Chemical Structure

CAS No. : 50847-11-5

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 ￥500 In-stock
10 mg ￥450 In-stock
50 mg ￥650 In-stock
100 mg ￥880 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Ibudilast 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Pyroptosis Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Alzheimer’s Disease Compound Library
  • Neuroprotective Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[1].

IC50 & Target

phosphodiesterase[1]
体外研究
(In Vitro)

Ibudilast (1~100 μM; 24 hours; microglia) suppresses both IL-1β and IL-6 production at 100 µM, and significantly suppresses TNF-α production at 10 and 100 µM[1].
Ibudilast (1~100 μM; 48 hours; neuronal cells) significantly increases the neuronal survival rate. Ibudilast (1~100 μM; 48 hours; microglia) inhibits the production of superoxide and NO[1].
Ibudilast upregulates the production of IL-10 in a dose-dependent manner. Ibudilast increases NGF mRNA and protein levels and GDNF and NT-4 mRNA expression. Ibudilast decreases the apoptotic changes observed in the neuronal cells in a dose-dependent manner[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.

Western Blot Analysis[1]

Cell Line: Microglia
Concentration: 1~100 μM
Incubation Time: 24 hours
Result: Suppressed both IL-1β and IL-6 production at 100 µM, and significantly suppresses TNF-α production at 10 and 100 µM.  

Clinical Trial

分子量

230.31

Formula

C14H18N2O
CAS 号

50847-11-5
中文名称

异丁司特；依布拉特；依布司特；异丁斯特
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 : ≥ 140 mg/mL (607.88 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 4.3420 mL 21.7099 mL 43.4197 mL
5 mM 0.8684 mL 4.3420 mL 8.6839 mL
10 mM 0.4342 mL 2.1710 mL 4.3420 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: ≥ 2.67 mg/mL (11.59 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (11.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 26.7 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: ≥ 2.67 mg/mL (11.59 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (11.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 26.7 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: ≥ 2.67 mg/mL (11.59 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (11.59 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 26.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 4.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

  • 5.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

  • 6.

    请依序添加每种溶剂： 1% DMSO    99% saline

    Solubility: 0.5 mg/mL (2.17 mM); Suspended solution; Need ultrasonic

*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]. Mizuno T, et al. Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia. Neuropharmacology. 2004 Mar;46(3):404-11.

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

生物活性分子抑制剂Ibudilast(Synonyms: 异丁司特; KC-404; AV-411; MN-166)

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。
Ibudilast (Synonyms: 异丁司特; KC-404; AV-411; MN-166) 纯度: 99.89%

Ibudilast (KC-404; AV-411; MN-166) 是一种环腺苷酸磷酸二酯酶 (PDE) 抑制剂。Ibudilast 具有抗血小板聚集作用。Ibudilast 抑制气管平滑肌收缩性，可用于哮喘的研究。Ibudilast 可能是一种有效的神经保护和抗痴呆药物，可对抗活化小胶质细胞的神经毒性。

Ibudilast(Synonyms: 异丁司特; KC-404; AV-411; MN-166)

Ibudilast Chemical Structure

CAS No. : 50847-11-5

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 ￥500 In-stock
10 mg ￥450 In-stock
50 mg ￥650 In-stock
100 mg ￥880 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Ibudilast 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Pyroptosis Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Alzheimer’s Disease Compound Library
  • Neuroprotective Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[1].

IC50 & Target

phosphodiesterase[1]
体外研究
(In Vitro)

Ibudilast (1~100 μM; 24 hours; microglia) suppresses both IL-1β and IL-6 production at 100 µM, and significantly suppresses TNF-α production at 10 and 100 µM[1].
Ibudilast (1~100 μM; 48 hours; neuronal cells) significantly increases the neuronal survival rate. Ibudilast (1~100 μM; 48 hours; microglia) inhibits the production of superoxide and NO[1].
Ibudilast upregulates the production of IL-10 in a dose-dependent manner. Ibudilast increases NGF mRNA and protein levels and GDNF and NT-4 mRNA expression. Ibudilast decreases the apoptotic changes observed in the neuronal cells in a dose-dependent manner[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.

Western Blot Analysis[1]

Cell Line: Microglia
Concentration: 1~100 μM
Incubation Time: 24 hours
Result: Suppressed both IL-1β and IL-6 production at 100 µM, and significantly suppresses TNF-α production at 10 and 100 µM.  

Clinical Trial

分子量

230.31

Formula

C14H18N2O
CAS 号

50847-11-5
中文名称

异丁司特；依布拉特；依布司特；异丁斯特
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 : ≥ 140 mg/mL (607.88 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 4.3420 mL 21.7099 mL 43.4197 mL
5 mM 0.8684 mL 4.3420 mL 8.6839 mL
10 mM 0.4342 mL 2.1710 mL 4.3420 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: ≥ 2.67 mg/mL (11.59 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (11.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 26.7 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: ≥ 2.67 mg/mL (11.59 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (11.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 26.7 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: ≥ 2.67 mg/mL (11.59 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (11.59 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 26.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 4.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

  • 5.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

  • 6.

    请依序添加每种溶剂： 1% DMSO    99% saline

    Solubility: 0.5 mg/mL (2.17 mM); Suspended solution; Need ultrasonic

*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]. Mizuno T, et al. Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia. Neuropharmacology. 2004 Mar;46(3):404-11.

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

Ibudilast-d7(Synonyms: 异丁司特 d7)

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。

Ibudilast-d7 (Synonyms: 异丁司特 d7)

Ibudilast-d7 是 Ibudilast 的氘代物。Ibudilast (KC-404; AV-411; MN-166) 是一种环腺苷酸磷酸二酯酶 (PDE) 抑制剂。Ibudilast 具有抗血小板聚集作用。Ibudilast 抑制气管平滑肌收缩性，可用于哮喘的研究。Ibudilast 可能是一种有效的神经保护和抗痴呆药物，可对抗活化小胶质细胞的神经毒性。

Ibudilast-d7(Synonyms: 异丁司特 d7)

Ibudilast-d7 Chemical Structure

CAS No. : 2713301-45-0

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

Ibudilast-d7 is the deuterium labeled Ibudilast. Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

237.35

Formula

C14H11D7N2O
CAS 号

2713301-45-0
中文名称

异丁司特 d7
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Mizuno T, et al. Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia. Neuropharmacology. 2004 Mar;46(3):404-11.

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