rTRD01
Based on 1 Customer Validation
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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- Purity: 99.10%
- CAS No.: 1332175-56-0
- 화학식: C18H21FN4O2
- 분자량:344.38
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Anti-Alzheimer's Disease Compound Library
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Neuroprotective Compound Library
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Radioprotector Library
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
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Anti-Fibrosis Compound Library
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
Kd: 89 uM (TDP-43102–269)[1]
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.
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.
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Animal Model:D42 GAL4 driver line (crossed with w1118 genetic background control, or lines expressing human TDP-43G298S/TDP-43WT; motor neuron expression of human G298S mutant TDP-43 via GAL4-UAS system)[1]
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Dosage:20 μM
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Administration:feeding; single exposure
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Result:Reduced larval turning time in TDP-43G298S-expressing larvae from 19.3 s to 12.3 s.
Showed no significant improvement in larval turning time in TDP-43WT-expressing larvae.
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Animal Model:Tübingen driver line (TDL6)[2]
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Dosage:10 μM, 25 μM, 50 μM, 75 μM
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Administration:incubated in E3 medium; starting at 12 hpf; media refreshed every 24 hours (co-treatment); washed at 18 hpf (sequential treatment)
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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
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CAS No. 1332175-56-0
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Appearance Solid
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분자량 344.38
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화학식 C18H21FN4O2
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Color Light yellow to yellow
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SMILES
O=C(C1=CN=CC(N2CCCC(CC3=CC=C(C=C3)F)(C2)CO)=N1)N
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (273 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |
rTRD01 Related Classifications
HY-153898 Related Classifications
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