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TPT-260

CAS# 769856-81-7

TPT-260

2D Structure

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TPT-260

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Chemical Properties of TPT-260

Cas No. 769856-81-7 SDF Download SDF
PubChem ID 414147 Appearance Powder
Formula C8H12N4S3 M.Wt 260.4
Type of Compound N/A Storage Desiccate at -20°C
Synonyms TPU260
Solubility >8.9mg/mL in DMSO
Chemical Name [5-(carbamimidoylsulfanylmethyl)thiophen-2-yl]methyl carbamimidothioate
SMILES C1=C(SC(=C1)CSC(=N)N)CSC(=N)N
Standard InChIKey XGDUNTSTRCLVLN-UHFFFAOYSA-N
Standard InChI InChI=1S/C8H12N4S3/c9-7(10)13-3-5-1-2-6(15-5)4-14-8(11)12/h1-2H,3-4H2,(H3,9,10)(H3,11,12)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of TPT-260

DescriptionTPT-260(TPU260) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, we temporally call this molecule as TPT-260. IC50 value: Target:

TPT-260 Dilution Calculator

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TPT-260 Molarity Calculator

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Preparing Stock Solutions of TPT-260

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.8402 mL 19.2012 mL 38.4025 mL 76.8049 mL 96.0061 mL
5 mM 0.768 mL 3.8402 mL 7.6805 mL 15.361 mL 19.2012 mL
10 mM 0.384 mL 1.9201 mL 3.8402 mL 7.6805 mL 9.6006 mL
50 mM 0.0768 mL 0.384 mL 0.768 mL 1.5361 mL 1.9201 mL
100 mM 0.0384 mL 0.192 mL 0.384 mL 0.768 mL 0.9601 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on TPT-260

TPT-260(TPU260) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, we temporally call this molecule as TPT-260.

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References on TPT-260

Retrograde transport of gamma-secretase from endosomes to the trans-Golgi network regulates Abeta42 production.[Pubmed:29851073]

J Neurochem. 2018 Oct;147(1):110-123.

The aberrant metabolism of amyloid-beta protein (Abeta) in the human brain has been implicated in the etiology of Alzheimer disease (AD). gamma-Secretase is the enzyme that generates various forms of Abeta, such as Abeta40 and Abeta42, the latter being an aggregation-prone toxic peptide that is involved in the pathogenesis of AD. Recently, we found that clathrin-mediated endocytosis of gamma-secretase affects the production and deposition of Abeta42 in vivo, suggesting that the membrane trafficking of gamma-secretase affects its enzymatic activity. However, the detailed intracellular trafficking pathway of gamma-secretase and its contribution to Abeta42 generation remain unclear. Here, we show that Retro-2, which inhibits the retrograde transport, elevated the Abeta42-generating activity both in cultured cells and mice brain. However, the result of in vitro gamma-secretase assay using a recombinant substrate suggested that Retro-2 did not elevate the intrinsic Abeta42-production activity of gamma-secretase. Immunocytochemistry and cell-surface biotinylation experiments revealed that gamma-secretase is recycled via the endosome-to-trans-Golgi network transport. In addition, gamma-secretase is retrogradely transported by syntaxin 5/6, known as targets of Retro-2, independent pathway. Conversely, TPT-260, which enhances the trafficking function of retromers, lowered Abeta42 levels and the Abeta42/(Abeta40 + Abeta42) ratio in secreted Abeta from cultured cells. Our results strongly suggest that the endosome-to-trans-Golgi network trafficking of gamma-secretase regulates its Abeta42 production activity. Modulation of this trafficking pathway might be a potential target for the development of Abeta42-lowering AD therapeutics. OPEN PRACTICES: Open Science: This manuscript was awarded with the Open Materials Badge. For more information see: https://cos.io/our-services/open-science-badges/.

Description

TPT-260(TPU260) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, we temporally call this molecule as TPT-260.

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