Art. -Nr.: HY-153898

rTRD01

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rTRD01 is an orally active, specific TDP-43 binder that targets the RRM1 and RRM2 domains of TDP-43. rTRD01 partially disrupts the interaction between TDP-43 and c9orf72 repeat RNA, but does not affect the binding of TDP-43 to canonical binding sequences. rTRD01 exhibits significant neuroprotective effects in zebrafish models, improves motor function and protects against paraquat (a widely used herbicide)-induced neurodegeneration, with no teratogenicity at high concentrations. rTRD01 is not a general antioxidant and cannot counteract Rotenone (HY-B1756)-induced neuronal death. rTRD01 can be used to study amyotrophic lateral sclerosis and other TDP-43 proteinopathies.

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Reinheit: 99.10%
CAS. Nr.: 1332175-56-0
Formel: C₁₈H₂₁FN₄O₂
Molecular Weight:344.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

rTRD01 Chemical Structure

CAS. Nr.: 1332175-56-0

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Kd: 89 uM (TDP-43_102–269)^[1]

In Vitro

rTRD01 (500 μM) binds specifically to recombinantly purified human TDP-43(102-269)-His protein^[1].
rTRD01 (0.03 μM-1 mM) binds to recombinantly purified human TDP-43(102-269)-His protein with an apparent dissociation constant of 89.4 μM, as measured by MST^[1].
rTRD01 (0.01 mM-1 mM; 30 min pre-incubation with TDP-43 proteins, 90 min incubation with RNA) selectively inhibits the interaction of recombinantly purified human TDP-43 proteins with disease-linked (GGGGCC)₄ c9orf72 RNA, with an IC₅₀ of ~150 μM for TDP-43(102-269)-His, while sparing interactions with canonical (UG)₆ RNA^[1].
rTRD01 binds to the RNA recognition motifs of human TDP-43 and partially disrupts its interaction with disease-associated (GGGGCC)₄ RNA^[2].

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

In Vivo

rTRD01 (20 μM; feeding; single exposure) significantly reduces ALS-like locomotor defects in Drosophila larvae expressing TDP-43^G298S mutant, decreasing larval turning time from 19.3 s-12.3 s^[1].
rTRD01 (10-75 μM; incubated in E3 medium; starting at 12 hpf) protects against paraquat-induced neurodegeneration in zebrafish embryos by a non-general antioxidant mechanism, as evidenced by rescue of spinal curvature and brain morphology metrics with no effect on rotenone-induced neuronal death^[2].

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

Animal Model:

D42 GAL4 driver line (crossed with w¹¹¹⁸ genetic background control, or lines expressing human TDP-43^G298S/TDP-43^WT; motor neuron expression of human G298S mutant TDP-43 via GAL4-UAS system)^[1]
Dosage:

20 μM
Administration:

feeding; single exposure
Result:

Reduced larval turning time in TDP-43^G298S-expressing larvae from 19.3 s to 12.3 s.
Showed no significant improvement in larval turning time in TDP-43^WT-expressing larvae.

Animal Model:

Tübingen driver line (TDL6)^[2]
Dosage:

10 μM, 25 μM, 50 μM, 75 μM
Administration:

incubated in E3 medium; starting at 12 hpf; media refreshed every 24 hours (co-treatment); washed at 18 hpf (sequential treatment)
Result:

Reduced spine deformity prevalence from ~70% with paraquat alone to ~10% with 50 μM rTRD01 co-treatment or sequential treatment.
Eliminated statistically significant reductions in brain cross-sectional area, mean fluorescence, and fluorescence density caused by paraquat alone with 50 μM rTRD01 co-treatment.
Showed no protective effect against rotenone-induced gray brain phenotype at doses of 10, 25, 50, or 75 μM.
Was well-tolerated up to 75 μM, with no discernable morphological defects and >90% survival through 5 dpf at all tested doses.

Chemical Information

CAS. Nr. 1332175-56-0
Appearance Solid
Molecular Weight 344.38
Formel C₁₈H₂₁FN₄O₂
Color Light yellow to yellow
SMILES

O=C(C1=CN=CC(N2CCCC(CC3=CC=C(C=C3)F)(C2)CO)=N1)N
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (290.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9038 mL

14.5188 mL

29.0377 mL

5 mM

0.5808 mL

2.9038 mL

5.8075 mL

10 mM

0.2904 mL

1.4519 mL

2.9038 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. François-Moutal L, et al. Small Molecule Targeting TDP-43's RNA Recognition Motifs Reduces Locomotor Defects in a Drosophila Model of Amyotrophic Lateral Sclerosis (ALS). ACS Chem Biol. 2019;14(9):2006-2013. [Content Brief]

[2]. Jahanbakhsh S. Chemical Biology Approaches to Modeling and Treating Brain Disease[M]. University of California, Los Angeles, 2019.

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9038 mL	14.5188 mL	29.0377 mL	72.5942 mL
	5 mM	0.5808 mL	2.9038 mL	5.8075 mL	14.5188 mL
	10 mM	0.2904 mL	1.4519 mL	2.9038 mL	7.2594 mL
	15 mM	0.1936 mL	0.9679 mL	1.9358 mL	4.8396 mL
	20 mM	0.1452 mL	0.7259 mL	1.4519 mL	3.6297 mL
	25 mM	0.1162 mL	0.5808 mL	1.1615 mL	2.9038 mL
	30 mM	0.0968 mL	0.4840 mL	0.9679 mL	2.4198 mL
	40 mM	0.0726 mL	0.3630 mL	0.7259 mL	1.8149 mL
	50 mM	0.0581 mL	0.2904 mL	0.5808 mL	1.4519 mL
	60 mM	0.0484 mL	0.2420 mL	0.4840 mL	1.2099 mL
	80 mM	0.0363 mL	0.1815 mL	0.3630 mL	0.9074 mL
	100 mM	0.0290 mL	0.1452 mL	0.2904 mL	0.7259 mL

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rTRD01

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Antioxidant Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

rTRD01

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Antioxidant Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

rTRD01 Related Classifications

HY-153898 Related Classifications