1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. Tasronetide

Tasronetide (FTX-101) is a highly selective inhibitor toward the NRP1/Plexin-A1 receptor system, and displays no significant activity on other targets. Tasronetide intercalates within the transmembrane domains of Plexin-A1 and NRP1 of oligodendrocytes, interferes with the heterodimerization of the co-receptor system, effectively disrupts the NRP1/Plexin-A1 receptor complex and mitigates the inhibitory influence of Sema3A on oligodendrocyte migration and differentiation, thereby facilitating increased myelin sheathing around axons. Tasronetide is designed to enhance the recruitment and maturation of oligodendrocyte precursors and can be used for Chronic Op c Neuropathy research.

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Tasronetide

Tasronetide Chemical Structure

CAS No. : 2919567-65-8

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Description

Tasronetide (FTX-101) is a highly selective inhibitor toward the NRP1/Plexin-A1 receptor system, and displays no significant activity on other targets. Tasronetide intercalates within the transmembrane domains of Plexin-A1 and NRP1 of oligodendrocytes, interferes with the heterodimerization of the co-receptor system, effectively disrupts the NRP1/Plexin-A1 receptor complex and mitigates the inhibitory influence of Sema3A on oligodendrocyte migration and differentiation, thereby facilitating increased myelin sheathing around axons. Tasronetide is designed to enhance the recruitment and maturation of oligodendrocyte precursors and can be used for Chronic Op c Neuropathy research[1].

IC50 & Target

NRP1/Plexin-A1 Receptor[1]

In Vitro

Tasronetide (1 h; 0.1-100 nM) disrupts the dimerization of Plexin-A1 with its co-receptor NRP1 in Oli-neu cell line (IC50 = 0.091 nM)[1].
Tasronetide (1 h; 10-100 nM) counteracted Sema3A inhibitory effect on the maturation of human fibroblast-derived oligodendrocytes[1].
Tasronetide (1 h; 0.1 nM-1 μM) blocked the inhibitory effect on migration induced by Sema3A in Oli-neu cells[1].
Tasronetide (6 h; 100 nM) counteracted Sema3A repulsive effect on migration induced by Sema3A in human fibroblast-derived oligodendrocytes (HFDO)[1].
Tasronetide’s (1 h; 0.1 nM-1 μM) pharmacological activity is dose-dependent with an IC50 of 1.2 nM on transmigration of Oli-neu cells[1].
Tasronetide (10 days; 100 nM) does not affect proliferation of HFDO[1].
Tasronetide (72 h; 0.01–10 µM) has no neurotoxic effects on primary mouse cortical neurons[1].
Tasronetide (5 weeks; 100 nM) potentiates myelination in co-culture fibroblast-derived oligodendrocytes and neuronal progenitor cells derived neurons by antagonizing the inhibitory effects of Sema3A signaling[1].

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

Real Time qPCR[1]

Cell Line: HFDO
Concentration: 10 nM plus Sema3A (100 ng/mL); 100 nM plus Sema3A (100 ng/mL)
Incubation Time: 1 h
Result: Restored MBP expression compared with Sema3A added alone group.

Cell Migration Assay [1]

Cell Line: Oli-neu cells
Concentration: 0.1 nM plus Sema3A (20 ng/mL); 1 nM plus Sema3A (20 ng/mL); 10 nM plus Sema3A (20 ng/mL); 100 nM plus Sema3A (20 ng/mL); 1 μM plus Sema3A (20 ng/mL)
Incubation Time: 1 h
Result: Blocked the inhibitory effect on migration induced by Sema3A restoring the migratory potential to that of the untreated control group.

Cell Migration Assay [1]

Cell Line: HFDO
Concentration: 100 nM; 100 nM plus Sema3A (100 ng/mL)
Incubation Time: 6 h
Result: Blocked the inhibitory effect on migration induced by Sema3A restoring the migratory potential to that of the untreated control group.

Cell Proliferation Assay[1]

Cell Line: HFDO
Concentration: 100 nM
Incubation Time: 10 days
Result: Did not affect cell proliferation.

Real Time qPCR[1]

Cell Line: HFDO
Concentration: 100 nM
Incubation Time: 16 days
Result: Unaffected the mRNA expression of Ki67.

Immunofluorescence[1]

Cell Line: Co-culture fibroblast-derived oligodendrocytes and neuronal progenitor cells derived neurons
Concentration: 10−4 M
Incubation Time: 5 weeks
Result: Completely blocked the Sema3A inhibitory effect on myelination.
Clinical Trial
Molecular Weight

3042.43

Formula

C138H225N29O47

CAS No.
Sequence

Thr-Leu-Pro-Ala-Ile-Thr-Gly-Leu-Val-Gly-Gly-Val-Gly-Leu-Leu-Leu-Glu-Val-Ile-Val-Glu-Val-Ala-Tyr-Glu-Glu-Glu-Glu-Glu

Sequence Shortening

TLPAITGLVGGVGLLLEVIVEVAYEEEEE

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Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tasronetide
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HY-P11272
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