1. Neuronal Signaling Apoptosis Immunology/Inflammation
  2. Amyloid-β Apoptosis CD47 Huntingtin
  3. SEN177

SEN177 是一种口服有效的谷氨酰胺环化酶 (QC) 抑制剂。SEN177 对人谷氨酰胺环化酶 (hQC) 的 Ki 为 20 nM,IC50 为 13 nM。SEN177 能干扰 CD47 与 SIRPα 相互作用,具有抗肿瘤的活性。SEN177 可降低亨廷顿模型中由于 HTT 突变导致的聚集和凋亡 (apoptosis),可用于神经退行性疾病的研究。

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SEN177 Chemical Structure

SEN177 Chemical Structure

CAS No. : 2117405-13-5

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10 mM * 1 mL in DMSO ¥1100
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5 mg ¥1000
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10 mg ¥1700
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SEN177 is an orally effect glutamine cyclase (QC) inhibitor. The Ki of SEN177 for human glutamine cyclase (hQC) is 20 nM, and the IC50 is 13 nM. SEN177 interferes with the interaction between CD47 and SIRRPα, and has anti-tumor activity. SEN177 reduces aggregation and apoptosis caused by HTT mutation in Huntington model, and can be used in the study of neurodegenerative diseases[1][2][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf21 IC50
16.7 nM
Compound: 4; SEN177
Inhibition of recombinant human N-terminal His6-tagged glutaminyl cyclase (Ala33 to Leu361 residues) expressed in baculovirus infected Sf21 insect cells using H-Gln-AMC hydrobromide as substrate measured in presence of pGAPase by fluorometric assay
Inhibition of recombinant human N-terminal His6-tagged glutaminyl cyclase (Ala33 to Leu361 residues) expressed in baculovirus infected Sf21 insect cells using H-Gln-AMC hydrobromide as substrate measured in presence of pGAPase by fluorometric assay
[PMID: 31411468]
体外研究
(In Vitro)

SEN177 (0-50 μM;0-96 小时) 在乳腺癌细胞系 MDA-MB-468 中可以有效阻断 CD47 与 SIRPα 的相互作用[2]
SEN177 (10 μM;3 天) 在食管鳞状细胞癌 (Kyse-30) 和乳腺癌细胞系 (MDA-MB-468) 中,显著增强了 EGFR 抗体诱导 ADCP 的能力[2]
SEN177 (50 μM;24 小时) 在表达 HTT (Q74) 的 HeLa 细胞中降低突变 HTT 聚集体比例和凋亡[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SEN177 (50 μM;口服;两天更换一次) 在亨廷顿果蝇模型中具有保护作用[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Drosophila expressing Httex1Q46 in the eye[3]
Dosage: 50 μM
Administration: Oral administration (p.o.); Change every two days
Result: Reduced the number of aggregates.
Rescued the number of visible rhabdomeres.
Prevented neurodegeneration.
分子量

338.38

Formula

C18H19FN6

CAS 号
性状

固体

颜色

Brown to gray

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 31.25 mg/mL (92.35 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9553 mL 14.7763 mL 29.5526 mL
5 mM 0.5911 mL 2.9553 mL 5.9105 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 97.10%

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9553 mL 14.7763 mL 29.5526 mL 73.8814 mL
5 mM 0.5911 mL 2.9553 mL 5.9105 mL 14.7763 mL
10 mM 0.2955 mL 1.4776 mL 2.9553 mL 7.3881 mL
15 mM 0.1970 mL 0.9851 mL 1.9702 mL 4.9254 mL
20 mM 0.1478 mL 0.7388 mL 1.4776 mL 3.6941 mL
25 mM 0.1182 mL 0.5911 mL 1.1821 mL 2.9553 mL
30 mM 0.0985 mL 0.4925 mL 0.9851 mL 2.4627 mL
40 mM 0.0739 mL 0.3694 mL 0.7388 mL 1.8470 mL
50 mM 0.0591 mL 0.2955 mL 0.5911 mL 1.4776 mL
60 mM 0.0493 mL 0.2463 mL 0.4925 mL 1.2314 mL
80 mM 0.0369 mL 0.1847 mL 0.3694 mL 0.9235 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SEN177
目录号:
HY-136780
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