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Ibiglustat {[allProObj[0].p_purity_real_show]}

货号:A417980 同义名: Venglustat; SAR402671

Ibiglustat是一种强效且选择性的葡萄糖基神经酰胺合成酶 (GCS) 抑制剂和神经酰胺葡萄糖转移酶抑制剂。

Ibiglustat 化学结构 CAS号:1401090-53-6
Ibiglustat 化学结构
CAS号:1401090-53-6
Ibiglustat 3D分子结构
CAS号:1401090-53-6
Ibiglustat 化学结构 CAS号:1401090-53-6
Ibiglustat 3D分子结构 CAS号:1401090-53-6
规格 价格 会员价 库存 数量
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Ibiglustat 纯度/质量文件 产品仅供科研

货号:A417980 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Transferase 其他靶点 纯度
Tipifarnib +++

FTase, IC50: 0.6 nM

99%+
Tolcapone +

COMT, Ki: 30 nM

99%+
Lonafarnib +++

H-ras, IC50: 1.9 nM

K-ras-4B, IC50: 2.8 nM

99%+
(E)-Daporinad ++++

NMPRTase, Ki: 0.4 nM

99%+
FTI-277 HCl ++++

FTase, IC50: 500 pM

98%
A 922500 ++

mouse DGAT-1, IC50: 24 nM

human DGAT-1, IC50: 7 nM

98%
Lomeguatrib ++

O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM

99%+
PF-04620110 +

DGAT1, IC50: 19 nM

99%
LB42708 +++

FTase (N-ras), IC50: 1.2 nM

FTase (K-Ras), IC50: 0.8 nM

98%
GGTI298 Trifluoroacetate 98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Ibiglustat 生物活性

描述 Ibiglustat is a potent and selective glucosylceramide synthase inhibitor and ceramide glucosyltransferase inhibitor.

Ibiglustat 细胞实验

Cell Line
Concentration Treated Time Description References
colonoids 5 μmol/L 24 hours Inhibition of glucosylceramide synthase (GCS) activity, reducing glucosylceramide levels, leading to colonoid bursting in the presence of BFT FASEB J. 2020 Dec;34(12):15922-15945
HCT116 cells 0.5 μM 72 hours Evaluate the inhibitory effect of Ibiglustat on NTMT1, showing significant reductions in me3-RCC1 and me3-SET levels at 1 μM J Med Chem. 2022 Sep 22;65(18):12334-12345
HEK293 cells 1 μM 3 days Evaluate the inhibitory effect of venglustat on me3-RCC1 and me3-SET in HEK293 cells, showing significant inhibition at 1 μM J Med Chem. 2023 Jan 26;66(2):1601-1615

Ibiglustat 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice GBA-related synucleinopathy model Oral 0.03% wt/wt 8 months To evaluate the effects of sustained GCS inhibition on disease pathologies, results showed venglustat significantly reduced glycosphingolipid accumulation and improved cognitive deficits. Sci Rep. 2021 Oct 22;11(1):20945
Mice Neurological Gaucher disease model Oral 15 mg Once daily for 1 year To evaluate the safety and tolerability of venglustat and measure changes in the concentration of glucosylceramide and glucosylsphingosine in CSF. Results showed detectable venglustat in CSF and sustained reductions in glucosylceramide and glucosylsphingosine concentrations in 10 patients. Brain. 2023 Feb 13;146(2):461-474
C57BL/6 mice Normal mice and CBE-induced Gaucher disease type 3 mouse model Intraperitoneal injection 10 mg/kg Once daily for 14 days Evaluate the effect of compound 17 in reducing brain glucosylceramide and glucosylsphingosine, results showed that at 10 mg/kg dose, compound 17 had comparable effects to venglustat, reducing brain GlcCer and glucosylsphingosine by 19% and 39%, respectively ACS Chem Neurosci. 2020 Oct 21;11(20):3464-3473
Mice GBA11/L444P knock-in mice Oral 60 mg/kg body weight/day Starting 1 week after injections until the day of death To assess the effect of venglustat on α-synuclein inclusion formation, showing no significant reduction in hippocampal or SNc α-synuclein inclusions. J Neurosci. 2023 Jan 18;43(3):501-521

Ibiglustat 参考文献

[1]Jarnes Utz JR, Kim S, et al. Infantile gangliosidoses: Mapping a timeline of clinical changes. Mol Genet Metab. 2017 Apr 29. pii: S1096-7192(17)30112-9.

[2]Bountouvi E, Papadopoulou A, et al. Novel NPC1 mutations with different segregation in two related Greek patients with Niemann-Pick type C disease: molecular study in the extended pedigree and clinical correlations. BMC Med Genet. 2017 May 4;18(1):51.

Ibiglustat 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.84mL

2.57mL

1.28mL

25.67mL

5.13mL

2.57mL

Ibiglustat 技术信息

CAS号1401090-53-6
分子式C20H24FN3O2S
分子量 389.49
SMILES Code O=C(O[C@@H]1CN2CCC1CC2)NC(C)(C3=CSC(C4=CC=C(F)C=C4)=N3)C
MDL No. MFCD28502073
别名 Venglustat; SAR402671; GZ/SAR402671; Genz-682452; GZ402671
运输蓝冰
InChI Key YFHRCLAKZBDRHN-MRXNPFEDSA-N
Pubchem ID 60199242
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 50 mg/mL(128.37 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
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