D-TLKIVWC TFA
Based on 1 Customer Validation
D-TLKIVWC TFA is a Tau depolymerizing agent (IC50 = 12.1 μM). D-TLKIVWC TFA depolymerizes Tau into benign, seed-incompetent fragments. D-TLKIVWC TFA rescues behavioral deficits in mouse models and protects neurons from Tau-induced toxicity. D-TLKIVWC TFA can be used for research on Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C41H67N9O9S·xC2HF3O2
- Molecular Weight:862.09 (free base)
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
33.5 μM
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Inhibition of AD brain-extracted tau fibril seeding in HEK293T tau biosensor cells stably expressing YFP-fused tau assessed by reduction of tau puncta after 24 hrs.
Inhibition of AD brain-extracted tau fibril seeding in HEK293T tau biosensor cells stably expressing YFP-fused tau assessed by reduction of tau puncta after 24 hrs.
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38691615 |
| N2a | EC50 |
21.1 μM
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Protection against tau K18+ aggregate-induced cytotoxicity in Neuro2a neuronal cells assessed by MTT viability after 24 hrs.
Protection against tau K18+ aggregate-induced cytotoxicity in Neuro2a neuronal cells assessed by MTT viability after 24 hrs.
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38691615 |
In Vitro
D-TLKIVWC (500 μM; 48 h) TFA reduces GT38-reactive AD-tau in a cell-free dot blot assay[1].
D-TLKIVWC (5-100 µM) TFA inhibits recombinant tau K18+ aggregation with an IC50 of 12.1 µM[2].
D-TLKIVWC (20-50 µM; 24 h) TFA reduces intracellular tau aggregates in HEK293 and HEK293T tau aggregation models[2].
D-TLKIVWC (5-100 µM) TFA blocks the seeding of AD-extracted tau in tau biosensor cells, with an IC50 of approximately 33.5 µM[2].
D-TLKIVWC (500 μM; 48 h at 37°C) TFA reduces GT38 reactive brain-derived tau fibrils[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells expressing 1N4R tau and HEK293T cells stably expressing EYFP-fused tau 1N4R P301S
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Concentration:20 or 50 µM (D-TLKIVWC transfection); 10 µM (MG132)
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Incubation Time:24 h (AD fibril seeding); 24 h (D-TLKIVWC transfection and incubation); 24 h (EYFP-tau incubation)
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Result:Tau content in both pellet and supernatant was reduced in a dose-dependent manner at 20 and 50 µM.
Coincubation with MG132 reduced the reduction in tau content.
In EYFP-tau 1N4R P301S cells, the number of fluorescent tau puncta decreased compared with PBS control cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PS19 transgenic mice (P301S mutant human tau; Prnp-MAPT*P301S PS19Vle/J, JAX #008169; 2-month-old male and 6-month-old female cohorts)[2]
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Dosage:10 mg/kg
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Administration:i.v. via tail vein; once weekly; for 10 weeks; starting 2 weeks after stereotaxic seeding; combined with intranasal mannitol
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Result:In tau-seeded PS19 mice (n = 13 per group; 8 male and 5 female mice per group), body-weight loss associated with late-stage tau pathology was prevented over the 10-week dosing period.
In the Barnes maze, PS19 mice showed shorter learning latency to find the escape hole than vehicle or naked MNP control PS19 mice.
In the probe trial, latency, target-hole entries, and search paths were comparable to wild-type mice and improved relative to PBS control PS19 mice.
In the novel object recognition test, PS19 mice explored the novel object longer than the familiar object and showed improved discriminatory index and discriminatory ratio versus vehicle control PS19 mice.
AT8 immunohistochemistry showed reduced phosphorylated tau pathology in CA1 and CA3 regions relative to vehicle or naked MNP control mice.
Western blot analysis showed decreased RIPA-soluble and RIPA-insoluble phosphorylated tau levels in PS19 mouse brain (n = 8 per group).
Chemical Information
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Appearance Solid
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Molecular Weight 862.09 (free base)
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Formula C41H67N9O9S·xC2HF3O2
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Sequence
d-{Thr-Leu-Lys-Ile-Val-Trp-Cys}
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Sequence Shortening
d-{TLKIVWC}
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Solvent & Solubility
In Vitro:
H2O : 10 mg/mL (ultrasonic and warming and heat to 37°C)
DMSO : ≥ 10 mg/mL
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
References
D-TLKIVWC TFA Related Classifications
HY-P11593A Related Classifications
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