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製品番号: HY-183557

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O-GlcNAcase-IN-6

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2407072-65-3
分子式: C₂₀H₂₅N₅O
分子量:351.45

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

O-GlcNAcase-IN-6 構造式

CAS 番号: 2407072-65-3

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
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生物活性

製品説明

体外実験

O-GlcNAcase-IN-6 (Compound 24) potently inhibits human OGA by directly binding to the active site of the enzyme, with an IC₅₀ value of 5.4 nM^[1].
O-GlcNAcase-IN-6 inhibits OGA activity in HEK293 cells with an IC₅₀ of 26 nM^[1].
O-GlcNAcase-IN-6 exhibits low in vitro MDR1-MDCK permeability of 0.7 × 10^-6 cm/s, a high P-glycoprotein (PgP) efflux ratio (> 28), a free plasma protein binding rate of 0.61, and a free brain tissue binding rate of 0.24^[1].

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

Parmacokinetics

Species	Dose	Route	C₀	T_1/2	V_dss	CL	AUC_0-inf	C_max	T_max	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 %

体内実験

O-GlcNAcase-IN-6 (Compound 24) (100 mg/kg; p.o.; single dose) induces a transient, significant elevation of brain O-GlcNAcylation levels in male CD1 mice, confirming in vivo OGA target engagement^[1].

MedChemExpress (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.

Related Protocols :

Alzheimer’s Disease Modeling

化学情報

CAS 番号 2407072-65-3
分子量 351.45
分子式 C₂₀H₂₅N₅O
SMILES

CC1=C(C(C(C)C)=NC=C1)NC2=C3C=CN(C3=CC=N2)CC(N(C)C)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Bouton J, et al. Discovery of 5‑Azaindole Inhibitors of O‑GlcNAcase for the Treatment of Alzheimer's Disease and Related Tauopathies. ACS Med Chem Lett. 2026;17(5):1096-1105. Published 2026 Apr 23. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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