C2303552计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
提供 ≥95% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
避光,-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Genz-123346 (free base) is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; inhibits GM1 with IC50 value of 14 nM. IC50: 14 nM (GM1)
Exposure of cells to Genz-123346 and to other GCS inhibitors at nontoxic concentrations can enhance the killing of tumor cells by cytotoxic anti-cancer agents. Genz-123346 and a few other GCS inhibitors are substrates for multi-drug resistance efflux pumps such as P-gp (ABCB1, gP-170). In cell lines selected to over-express P-gp or which endogenously express P-gp, chemosensitization by Genz-123346 is primarily due to the effects on P-gp function. Genz-123346(Genz) is an enhancer of autophagy flux.
In the Zucker diabetic fatty rat, Genz-123346 loared glucose and A1C levels and improved glucose tolerance. Drug treatment also prevented the loss of pancreatic beta-cell function and preserved the ability of the animals to secrete insulin. In the diet-induced obese mouse, treatment with Genz-123346 normalized A1C levels and improved glucose tolerance. The oral bioavailability of the drug is shown to be about 10% and 30% in mice and rats, respectively, with a half-life in plasma of 30-60 min. Genz-123346 treatment results in a dose-dependent reduction of renal GlcCer and GM3 levels that translates into effective inhibition of cystic disease. A direct effect of Genz-123346 on the Akt-mTOR signaling pathway is observed, with reduced phosphorylation of Akt and ribosomal protein S6.
Information
Genz-123346 is an inhibitor ofGL1 synthasethat blocks the conversion of ceramide to GL1, the first step in the biosynthesis of gangliosides and other glycosphingolipids.
规格
别名
Genz-123346 游离碱
英文别名
Glucosylceramide Synthase Inhibitor | Genz-123346 - CAS 491833-30-8 - Calbiochem | (1R,2R)-nonanoic acid[2-(2ʹ,3ʹ-dihydro-benzo [1, 4] dioxin-6ʹ-yl)-2-hydroxy-1-pyrrolidin-1-ylmethyl-ethyl]-amide | GL1 synthase Inhibitor | Genz-123346 | Genz123346
规格或纯度
≥95%
英文名称
Genz-123346 free base
储存条件
避光,-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥95%
名称和识别符
PubChem SID
分子类型
小分子
Isomeric SMILES
CCCCCCCCC(=O)N[C@H](CN1CCCC1)[C@@H](C2=CC3=C(C=C2)OCCO3)O
分子量
418.57
Reaxy-Rn
20242348
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20242348&ln=
技术文档
高级数据
产品属性
| ALogP | 4.264 |
|---|---|
| hba_count | 3 |
| HBD Count | 2 |
| Rotatable Bond | 12 |
关联靶点（人）
UGCG
Tclin
神经酰胺葡萄糖基转移酶(Ceramide glucosyltransferase)
(1 活性数据)
UGCG
Tclin
Ceramide glucosyltransferase
(308 活性数据)
HepG2
(196354 活性数据)
关联靶点（其它种属）
Hdac6
Histone deacetylase 6 (222 活性数据)
Rattus norvegicus (775804 活性数据)
rep
Replicase polyprotein 1ab (378 活性数据)
SARS-CoV-2 (38078 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
敏感性
对光敏感
DMSO(mg / mL) Max Solubility
84
DMSO(mM) Max Solubility
200.683278782521
Water(mg / mL) Max Solubility
＜1
分子量
418.600 g/mol
XLogP3
4.200
氢键供体数Hydrogen Bond Donor Count
2
氢键受体数Hydrogen Bond Acceptor Count
5
可旋转键计数Rotatable Bond Count
12
精确质量Exact Mass
418.283 Da
单同位素质量Monoisotopic Mass
418.283 Da
拓扑极表面积Topological Polar Surface Area
71.000 Ų
重原子数Heavy Atom Count
30
形式电荷Formal Charge
0
复杂度Complexity
498.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
2
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
1
质检证书（CoA,COO,BSE/TSE 和分析图谱)
溶液计算器
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