标签归档：lu

LU-32-176B

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。

LU-32-176B 

LU-32-176B 是一种 GABA transporter 1(GAT1) 选择性抑制剂，与 GAT2 转运抑制剂 EF1502 具有协同抗惊厥作用。LU-32-176B 抑制 neurons、astrocytes 和 mGAT1，IC50 值分别为 2μM，1μM 和 4μM。

LU-32-176B

LU-32-176B Chemical Structure

CAS No. : 770688-66-9

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

LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively[1][2].

IC50 & Target

LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively[1][2].
体内研究
(In Vivo)

LU-32-176B (i.p.) and EF1502 can prevent sound-induced seizures in the Frings AGS-susceptible mouse model[1].

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

398.45

Formula

C23H24F2N2O2
CAS 号

770688-66-9
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]. Schousboe A, et al. GABA transporters as drug targets for modulation of GABAergic activity. Biochem Pharmacol. 2004;68(8):1557-1563.

    [2]. White HS, et al. First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2. J Pharmacol Exp Ther. 2005;312(2):866-874.

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

LU-32-176B

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。

LU-32-176B 

LU-32-176B 是一种 GABA transporter 1(GAT1) 选择性抑制剂，与 GAT2 转运抑制剂 EF1502 具有协同抗惊厥作用。LU-32-176B 抑制 neurons、astrocytes 和 mGAT1，IC50 值分别为 2μM，1μM 和 4μM。

LU-32-176B

LU-32-176B Chemical Structure

CAS No. : 770688-66-9

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

LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively[1][2].

IC50 & Target

LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively[1][2].
体内研究
(In Vivo)

LU-32-176B (i.p.) and EF1502 can prevent sound-induced seizures in the Frings AGS-susceptible mouse model[1].

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

398.45

Formula

C23H24F2N2O2
CAS 号

770688-66-9
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]. Schousboe A, et al. GABA transporters as drug targets for modulation of GABAergic activity. Biochem Pharmacol. 2004;68(8):1557-1563.

    [2]. White HS, et al. First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2. J Pharmacol Exp Ther. 2005;312(2):866-874.

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

LU-32-176B

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。

LU-32-176B 

LU-32-176B 是一种 GABA transporter 1(GAT1) 选择性抑制剂，与 GAT2 转运抑制剂 EF1502 具有协同抗惊厥作用。LU-32-176B 抑制 neurons、astrocytes 和 mGAT1，IC50 值分别为 2μM，1μM 和 4μM。

LU-32-176B

LU-32-176B Chemical Structure

CAS No. : 770688-66-9

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

LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively[1][2].

IC50 & Target

LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively[1][2].
体内研究
(In Vivo)

LU-32-176B (i.p.) and EF1502 can prevent sound-induced seizures in the Frings AGS-susceptible mouse 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.
分子量

398.45

Formula

C23H24F2N2O2
CAS 号

770688-66-9
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]. Schousboe A, et al. GABA transporters as drug targets for modulation of GABAergic activity. Biochem Pharmacol. 2004;68(8):1557-1563.

    [2]. White HS, et al. First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2. J Pharmacol Exp Ther. 2005;312(2):866-874.

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

Sertindole(Synonyms: 舍吲哚; Lu 23-174)

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。

Sertindole (Synonyms: 舍吲哚; Lu 23-174) 纯度: 99.76%

Sertindole是5-HT2A，5-HT2C，D2和αl受体拮抗剂。

Sertindole(Synonyms: 舍吲哚; Lu 23-174)

Sertindole Chemical Structure

CAS No. : 106516-24-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥798 In-stock
10 mg ￥725 In-stock
50 mg ￥3283 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

Sertindole, a neuroleptic, is one of the newer antipsychotic medications available. Target: Multi-target In vitro studies showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole offers an alternative treatment option for refractory patients given its good EPS profile, favorable metabolic profile, and comparable efficacy to risperidone. Due to cardiovascular safety concerns, sertindole is available as a second-line choice for patients intolerant to other antipsychotic agents [1]. Sertindole should prove to be a very useful addition to the therapeutic options available for the treatment of psychotic disorders [2]. Sertindole improves negative symptoms, and is also effective for the treatment of neuroleptic-resistant schizophrenia. Sertindole is generally well tolerated and is associated with a low rate of extrapyramidal symptoms (EPS). Thus, sertindole is a useful option in the treatment of patients with schizophrenia [3].

IC50 & Target

5-HT2A Receptor

 

5-HT2C Receptor

 

Clinical Trial

分子量

440.94

Formula

C24H26ClFN4O
CAS 号

106516-24-9
中文名称

舍吲哚
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 : 25 mg/mL (56.70 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2679 mL 11.3394 mL 22.6788 mL
5 mM 0.4536 mL 2.2679 mL 4.5358 mL
10 mM 0.2268 mL 1.1339 mL 2.2679 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: ≥ 2.5 mg/mL (5.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.67 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 (5.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.67 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 (5.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.67 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Juruena, M.F., E.P. de Sena, and I.R. de Oliveira, Sertindole in the management of schizophrenia. J Cent Nerv Syst Dis, 2011. 3: p. 75-85.

    [2]. Kane, J.M. and C.A. Tamminga, Sertindole (Serdolect): preclinical and clinical findings of a new atypical antipsychotic. Expert Opin Investig Drugs, 1997. 6(11): p. 1729-41.

    [3]. Murdoch, D. and G.M. Keating, Sertindole : a review of its use in schizophrenia. CNS Drugs, 2006. 20(3): p. 233-55.

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