RI-AG03 acetate
Based on 1 Customer Validation
RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 acetate inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 acetate 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 acetate suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 acetate can be used for research on tau-related diseases such as Alzheimer's disease.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.22%
- Formel: C104H189N49O22·xC2H4O2
- Molecular Weight:2477.93 (free base)
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Speicherung:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Liposomes conjugated with RI-AG03 (75 μM; 4 h) acetate show significantly enhanced binding to SH-SY5Y cells[2].
RI-AG03 (20 µM; 24 h) acetate potently inhibits the aggregation of recombinant 306VQIVYK311, 275VQIINK280, and the mixed 306VQIVYK311 + 275VQIINK280 hexapeptides[3].
RI-AG03 (0.5-200 µM; 24 h) acetate 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) acetate 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) acetate 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) acetate 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) acetate ose-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).
Chemical Information
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Appearance Solid
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Molecular Weight 2477.93 (free base)
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Formel C104H189N49O22·xC2H4O2
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Color White to off-white
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Sequence
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 -
Sequence Shortening
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 -
Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 2.5 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Reinheit & Dokumentation
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Data Sheet (291 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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 Aug 9;27(16):5066. [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 Nov;20(11):7788-7804. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
RI-AG03 acetate Related Classifications
HY-P10861A Related Classifications
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