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Cat. No.: HY-141878

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di-Ellipticine-RIBOTAC

di-Ellipticine-RIBOTAC is a RNase recruiting chimera (RIBOTAC) degrader, capable of specifically binding and degrading expanded G4C2 RNA repeat (r(G₄C₂)^exp). di-Ellipticine-RIBOTAC selectively binds the three-dimensional (3D) structure formed by r(G₄C₂)^exp and that recruits an endogenous ribonuclease (RNase) to cleave r(G₄C₂)^exp. di-Ellipticine-RIBOTAC selectively degrades the mutant chromosome 9 open reading frame 72 (C9orf72) allele and reduces quantities of toxic dipeptide repeat proteins (DPRs) translated from r(G₄C₂)^exp. di-Ellipticine-RIBOTAC significantly improves the pathological phenotype of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) in cells and mouse models. di-Ellipticine-RIBOTAC can be used for the study of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD).

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CAS No.: 2767983-76-4
Formule: C₇₈H₈₇N₇O₁₆S
Masse moléculaire:1410.63

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

di-Ellipticine-RIBOTAC Chemical Structure

CAS No.: 2767983-76-4

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Use of MCE Products

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

Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis :

In Vitro

di-Ellipticine-RIBOTAC (compound 7) (5-500 nM) inhibits RAN translation of r(G₄C₂)66 in HEK293T cells, and reduces quantities of the r(G₄C₂)^exp-containing transcript in a dose-dependent fashion^[1].
di-Ellipticine-RIBOTAC (5-500 nM) selectively reduces C9orf72 intron 1 abundance with an IC₅₀ of ~50 nM. di-Ellipticine-RIBOTAC also reduces poly(GP) abundance in c9ALS patient-derived lymphoblastoid cell lines (LCLs) and c9ALS patient-derived induced pluripotent stem cells (iPSCs)^[1].
Di-Ellipticine-RIBOTAC (50 nM; 2.5 weeks) reduces C9orf72 transcripts containing the r(G₄C₂)^exp repeat in intron 1 in iPSC-derived spinal motor neurons (iPSNs) from c9ALS patients and reversed the loss of Nup98^[1].
di-Ellipticine-RIBOTAC cleaves Cy5- and Cy3-labeled r(G₄C₂)₈ RNA in the presence of RNase L^[1].
di-Ellipticine-RIBOTAC inhibits hnRNP H1 binding to r(G₄C₂)₈ RNA (IC₅₀ = 2.4 μM)^[1].

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

In Vivo

di-Ellipticine-RIBOTAC (compound 7) (33 nmol; i.c.v.; single dose) reduces c9ALS/FTD pathology in a C9orf72 bacterial artificial chromosome (BAC) mouse model (+/+PWR500^[1].

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

Animal Model:

+/+PWR500 (12-25 weeks old) (expressing 500 r(G4C2) repeats)^[1]
Dosage:

33 nmol
Administration:

i.c.v.; single dose
Result:

Reduced r(G₄C₂)^exp-containing intron 1 mRNA abundance by 44% compared to vehicle-treated controls, decreased the number of r(G₄C₂)^exp-containing nuclear foci, reduced poly(GP) abundance by 74% in brain tissue, decreased poly(GP) and poly(GA) aggregates, and decreased TDP-43 inclusions.

Chemical Information

CAS No. 2767983-76-4
Masse moléculaire 1410.63
Formule C₇₈H₈₇N₇O₁₆S
SMILES

CCOC(C1=C(S/C(C1=O)=C\C2=CC=C(C(O)=C2)OCCOCCOCCOCCNC(CCC(N(CCOCCOCCOC3=CC4=C(NC5=C4C(C)=C6C=NC=CC6=C5C)C=C3)CCOCCOCCOC7=CC=C8NC9=C(C(C)=C%10C=NC=CC%10=C9C)C8=C7)=O)=O)NC%11=CC=CC=C%11)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 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)
Instruction de manipulation (2659 KB)

Références

[1]. Bush JA, et al. Ribonuclease recruitment using a small molecule reduced c9ALS/FTD r(G4C2) repeat expansion in vitro and in vivo ALS models. Sci Transl Med. 2021 Oct 27;13(617):eabd5991. [Content Brief]

Calculators

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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.

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MOQ

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100 mg

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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di-Ellipticine-RIBOTAC

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis