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製品番号: HY-136766

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PGL-135

PGL-135 is a blood-brain barrier-permeable Huntingtin aggregation inhibitor. PGL-135 is applicable to research related to Huntington'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: 26278-83-1
分子式: C₉H₁₀N₂OS
分子量:194.25

保管条件:

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

PGL-135 構造式

CAS 番号: 26278-83-1

価格（税別）

Amount: USD 0.00

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Use of MCE Products

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

生物活性

製品説明

PGL-135 is a blood-brain barrier-permeable Huntingtin aggregation inhibitor. PGL-135 is applicable to research related to Huntington's disease^[1]^[2]^[3]^[4].

体外実験

PGL-135 (25-50 μM) inhibits the aggregation of HDQ51 in 293 Tet-Off cells expressing HDQ51, with an IC₅₀ of 40 μM; it reduces inclusion body formation by 30% at a concentration of 25 μM and by 50% at 50 μM^[2].

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

体内実験

PGL-135 (30 mg/kg; i.p.; single dose) crosses the blood-brain barrier but is rapidly metabolized in vivo, with undetectable levels in liver and near-undetectable levels in brain and serum by 40 minutes post-injection^[1].

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

Animal Model:

hemizygote R6/2 (female, 10-11 weeks old, CBA × C57BL/6 F1 background); wild-type littermates (female, 10-11 weeks old, CBA × C57BL/6 F1 background)^[1]
Dosage:

30 mg/kg
Administration:

i.p.; single dose
Result:

Was detectable in micromolar concentrations in brain and serum during the first 30 minutes post-injection.
Was virtually undetectable by 40 minutes post-injection.
Was not reliably detectable in liver at any time point.

化学情報

CAS 番号 26278-83-1
分子量 194.25
分子式 C₉H₁₀N₂OS
SMILES

OC1=CC(=C2N=C(SC2=C1C)N)C
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]. Hockly E, et al. Evaluation of the benzothiazole aggregation inhibitors riluzole and PGL-135 as therapeutics for Huntington's disease. Neurobiology of disease. 2006 Jan;21(1):228-36.

[2]. Ahamad S, et al. The Emerging Landscape of Small-Molecule Therapeutics for the Treatment of Huntington's Disease. J Med Chem. 2022 Dec 22;65(24):15993-16032.

[3]. Heiser V, et al. Identification of benzothiazoles as potential polyglutamine aggregation inhibitors of Huntington's disease by using an automated filter retardation assay. Proceedings of the National Academy of Sciences of the United States of America. 2002 Dec 10;99 Suppl 4(Suppl 4):16400-6.

[4]. Takahashi T, et al. Soluble polyglutamine oligomers formed prior to inclusion body formation are cytotoxic. Hum Mol Genet. 2008 Feb 1;17(3):345-56.

Calculators

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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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100 mg

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