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Cat. No.: 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.

For research use only. We do not sell to patients.

CAS No.: 26278-83-1
Formula: C₉H₁₀N₂OS
Molecular Weight:194.25

Storage:

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

PGL-135 Chemical Structure

CAS No.: 26278-83-1

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

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].

In Vitro

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.

In Vivo

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.

Chemical Information

CAS No. 26278-83-1
Molecular Weight 194.25
Formula C₉H₁₀N₂OS
SMILES

OC1=CC(=C2N=C(SC2=C1C)N)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

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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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