TGN-020


Catalog No. Size PriceQuantity
M11620-2 2mg solid $95
M11620-10 10mg solid $285

Description

TGN-020 is a selective Aquaporin 4 (AQP4) inhibitor with an IC50 of 3.1 μM. TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.TGN-020 alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats.

Product information

CAS Number: 51987-99-6

Molecular Weight: 206.22

Formula: C8H6N4OS

Chemical Name: N-(1, 3, 4-thiadiazol-2-yl)pyridine-3-carboxamide

Smiles: O=C(NC1=NN=CS1)C1=CN=CC=C1

InChiKey: AGEGZHOPKZFKBP-UHFFFAOYSA-N

InChi: InChI=1S/C8H6N4OS/c13-7(6-2-1-3-9-4-6)11-8-12-10-5-14-8/h1-5H,(H,11,12,13)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 16.67 mg/mL (80.84 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

In Vivo:

TGN-020 (0.02 mg/μL; two microliter intravitreal injections) can suppress retinal edema in STZ-induced diabetic rats (nine-week-old male Wistar rats) retinas. TGN-020 (100 mg/kg; ip; single dose immediately followed SCI) promotes functional recovery at days 3, 7, 14, 21, and 28, as well as reduces the degree of edema and inhibits the expression of AQP4, GFAP, PCNA at days 3 after SCI. TGN-020 inhibits the glial scar formation and upregulates GAP-43 expression in adult female Sprague-Dawley rats (180-220 g, 9-10 weeks old) with SCI.

References:

  1. Vincent J Huber, et al. Identification of aquaporin 4 inhibitors using in vitro and in silico methods. Bioorg Med Chem. 2009 Jan 1;17(1):411-7.
  2. Shou Oosuka, et al. Effects of an Aquaporin 4 Inhibitor, TGN-020, on Murine Diabetic Retina. Int J Mol Sci. 2020 Mar 27;21(7):2324.
  3. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

Products are for research use only. Not for human use.

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