RI-AG03
RI-AG03 is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 can be used for research on tau-related diseases such as 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。
- 分子式: C104H189N49O22
- 分子量:2477.93
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
Liposomes conjugated with RI-AG03 (75 μM; 4 h) show significantly enhanced binding to SH-SY5Y cells[2].
RI-AG03 (20 µM; 24 h) potently inhibits the aggregation of recombinant 306VQIVYK311, 275VQIINK280, and the mixed 306VQIVYK311 + 275VQIINK280 hexapeptides[3].
RI-AG03 (0.5-200 µM; 24 h) dose-dependently inhibits heparin-induced aggregation of recombinant TauΔ1-250, with an IC50 of 7.83 µM[3].
RI-AG03 (0.5-200 µM; 216 h) inhibits heparin-induced aggregation of recombinant full-length Tau2N4R in a dose-dependent manner, with an IC50 of 5 µM[3].
RI-AG03 (20 µM; 24 h) inhibits the formation of recombinant TauΔ1-250 fibrils and instead promotes the formation of large spherical amorphous aggregates[3].
RI-AG03 (20 µM; 5 h) reduces the conversion of recombinant TauΔ1-250 from a disordered random coil structure to β-sheet-rich aggregates[3].
RI-AG03 (0.5-500 µM; 16 h preincubation, 24 h cell incubation) dose-dependently inhibits the seeding aggregation of preformed Tau2N4R fibrils in HEK-293 Tau biosensor cells, with an IC50 of 23.85 µM, and shows no toxicity at effective doses up to 100 µM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GMR-GAL4 driver, UAS-Tau2N4R, ElavC155-GAL4 driver, Oregon-R[3]
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Dosage:0.08 µM, 0.8 µM, 20 µM, 40 µM
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Administration:oral; continuous; lifespan or 6 weeks
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Result:Significantly improved eye size in GMR-hTau2N4R flies compared to untreated controls (40 µM).
Partially rescued the Tau-induced rough-eye phenotype, improving bristle number/morphology and reducing abnormal ommatidia; ommatidial disorganization was significantly reduced (20 µM).
Increased median survival of pan-neuronal hTau2N4R flies from 26 to 35 days (35% improvement; 0.8 µM).
Increased median survival of pan-neuronal hTau2N4R flies from 26 to 33 days (27% improvement; 0.08 µM).
Reduced total Tau aggregates (oligomers and fibrils) by 73% in pan-neuronal hTau2N4R flies; treated flies showed no fibrillar species, only large amorphous structures ~30-50 nm in diameter (0.08 µM).
化学情報
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分子量 2477.93
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分子式 C104H189N49O22
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配列
Ac-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-Gly-{d-Pro}-{d-Lys}-{d-Tyr}-{d-Lys
}-{D-Ile}-{d-Gln}-{d-Val}-Gly-{d-Arg}-NH2 -
シーケンスの短縮
Ac-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-G-{d-Pro}-{d-Lys}-{d-Tyr}-{d-Lys
}-{D-Ile}-{d-Gln}-{d-Val}-G-{d-Arg}-NH2 -
輸送条件
Room temperature in continental US; may vary elsewhere.
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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
参考文献
[1]. Di Natale G, et al. Aβ and Tau Interact with Metal Ions, Lipid Membranes and Peptide-Based Amyloid Inhibitors: Are These Common Features Relevant in Alzheimer's Disease?. Molecules. 2022;27(16):5066. Published 2022 Aug 9. [Content Brief]
[2]. Reich N, et al. Liposome nanoparticle conjugation and cell penetrating peptide sequences (CPPs) enhance the cellular delivery of the tau aggregation inhibitor RI-AG03. J Cell Mol Med. 2024;28(11):e18477. [Content Brief]
[3]. Aggidis A, et al. A novel peptide-based tau aggregation inhibitor as a potential therapeutic for Alzheimer's disease and other tauopathies. Alzheimers Dement. 2024;20(11):7788-7804. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
RI-AG03 関連分類
HY-P10861 関連分類
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