2. Neuronal Signaling
  3. OGA
  4. O-GlcNAcase-IN-6

O-GlcNAcase-IN-6 是一种口服有效的、可穿过血脑屏障的 O-GlcNAcase (OGA) 抑制剂，其 IC50 为 5.4 nM。O-GlcNAcase-IN-6 可抑制 OGA 活性，进而导致脑组织中 O-GlcNAc 糖基化水平升高。O-GlcNAcase-IN-6 可用于阿尔茨海默病的研究。

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O-GlcNAcase-IN-6

O-GlcNAcase-IN-6 Chemical Structure

CAS No. : 2407072-65-3

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O-GlcNAcase-IN-6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

O-GlcNAcase-IN-6 is an orally active, blood-brain barrier-permeable O-GlcNAcase (OGA) inhibitor with an IC50 of 5.4 nM. O-GlcNAcase-IN-6 inhibits OGA activity, thereby increasing the level of O-GlcNAc glycosylation in brain tissues. O-GlcNAcase-IN-6 can be used for the research of Alzheimer's disease[1].

体外研究
(In Vitro)

O-GlcNAcase-IN-6 (Compound 24) 可通过直接结合酶的活性位点强效抑制人源 OGA，其 IC50 为 5.4 nM[1]。
O-GlcNAcase-IN-6 可抑制 HEK293 细胞中的 OGA 活性，其 IC50 为 26 nM[1]。
O-GlcNAcase-IN-6 具有较低的体外 MDR1-MDCK 通透性，为 0.7 × 10-6 cm/s，PgP 外排率较高 (> 28)，游离血浆蛋白结合率为 0.61，游离脑组织结合率为 0.24[1]。

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

O-GlcNAcase-IN-6 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route C0 T1/2 Vdss CL AUC0-inf Cmax Tmax Bioavailability
Mice[1] 1 mg/kg i.v. 794 ng/mL 1.02 h 2.1 L/kg 50 mL/min/kg 338 ng·h/mL / / /
Mice[1] 5 mg/kg p.o. / 1.7 h / / 1793 ng·h/mL 697 ng/mL 0.5 h 100 %
体内研究
(In Vivo)

O-GlcNAcase-IN-6 (Compound 24) (100 mg/kg；口服；单次给药) 可使雄性 CD1 小鼠脑内 O-GlcNAcylation 水平短暂且显著升高，证实其在体内与 OGA 靶点结合[1]。

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

Animal Model: CD1 mice (male)[1]
Dosage: 100 mg/kg
Administration: p.o.; single dose
Result: Induced a transient elevation of brain O-GlcNAcylation levels, peaking at 8 hours post-administration.
Reached a peak increase similar to the 3-3.5-fold increase observed with the reference compound Thiamet-G (500 mg/kg).
Showed measurable brain exposure, with an AUC(brain)/AUC(plasma) ratio of 0.16 and an unbound brain-to-plasma partition coefficient (Kp,uu) of 0.07.
分子量

351.45

Formula

C20H25N5O
CAS 号
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.
纯度 & 产品资料
参考文献

O-GlcNAcase-IN-6 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

O-GlcNAcase-IN-62407072-65-3OGAO-GlcNAc hydrolaseO-GlcNAcasebrain tissuemurine modelsMDR1-MDCKhuman liver microsomesmouse liver microsomesHEK293 cellsalzheimer’s diseasemale CD1 miceInhibitorinhibitorinhibit

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