MedKoo Cat#: 504210 | Name: TPT-260 2HCl (R55)
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

TPT-260 2HCl, also known as R55, 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. TPT260 acts as a chaperone to stabilize the retromer complex against thermal denaturation (Kd = ~ 5 µM). In cultured hippocampal neurons, TPT-260 dose-dependently increases the level of retromer proteins, redirects APP from the endosome, and reduces the formation of pathogenic APP. **** Please also see similar products: TPT-197; TPT-260; TPT-172.

Chemical Structure

TPT-260 2HCl (R55)
TPT-260 2HCl (R55)
CAS#2076-91-7 (2HCl)

Theoretical Analysis

MedKoo Cat#: 504210

Name: TPT-260 2HCl (R55)

CAS#: 2076-91-7 (2HCl)

Chemical Formula: C8H14Cl2N4S3

Exact Mass: 0.0000

Molecular Weight: 333.31

Elemental Analysis: Elemental Analysis: C, 28.83; H, 4.23; Cl, 21.27; N, 16.81; S, 28.86

Price and Availability

Size Price Availability Quantity
5mg USD 70.00 Ready to ship
10mg USD 120.00 Ready to ship
25mg USD 150.00 Ready to ship
100mg USD 450.00 Ready to ship
200mg USD 750.00 Ready to ship
500mg USD 1,550.00 Ready to ship
1g USD 2,650.00 Ready to ship
2g USD 4,750.00 Ready to ship
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Related CAS #
769856-81-7 (free base) 2076-91-7 (2HCl)
Synonym
TPT260; TPT-260; TPT 260; TPT-260 HCl; TPT-260 2HCl; TPT-260 dihydrchloride; R55. NSC-55712; NSC55712; NSC 55712
IUPAC/Chemical Name
thiophene-2,5-diylbis(methylene) dicarbamimidothioate dihydrochloride
InChi Key
DSODRWWHAUGSGD-UHFFFAOYSA-N
InChi Code
InChI=1S/C8H12N4S3.2ClH/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);2*1H
SMILES Code
NC(SCC1=CC=C(CSC(N)=N)S1)=N.[H]Cl.[H]Cl
Appearance
White to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO and in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
TPT-260 is a thiophene thiourea derivative that acts as a chaperone to stabilize the retromer complex against thermal denaturation.
In vitro activity:
γ-Secretase located at late endosomes/lysosomes exhibited higher Aβ42 production activity than γ-secretase localized in other compartments. Thus, the enhanced retrieval of γ-secretase from late endosomes/lysosomes would lead to a decrease in the Aβ42/(Aβ40 + Aβ42) production ratio. TPT-260 treatment reduced sAPPβ production without affecting the levels of APP nor BACE1. Notably, TPT-260 treatment caused a reduction not only in secreted Aβ levels but the Aβ42/(Aβ40 + Aβ42) ratio (Fig. 6a and b). Furthermore, the accumulation of mNct was also observed in TPT-260-treated cells (Fig. 6c and d). Considering the result, that TPT-260 treatment increased the co-localization of A5226A and TGN46 (Fig. 4d), these data suggest that TPT-260 acts as a novel Aβ42-lowering GSM targeting endosome-to-TGN retrograde transport. Collectively, these results strongly suggest that the rate of the endosome-to-TGN transport of γ-secretase is closely associated with the production ratio of Aβ42/(Aβ40 + Aβ42). Reference: J Neurochem. 2018 Oct; 147(1): 110-123. https://onlinelibrary.wiley.com/doi/full/10.1111/jnc.14477
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 62.5 240.02
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 333.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
Kanatsu K, Hori Y, Ebinuma I, Chiu YW, Tomita T. Retrograde transport of γ-secretase from endosomes to the trans-Golgi network regulates Aβ42 production. J Neurochem. 2018 Oct;147(1):110-123. doi: 10.1111/jnc.14477. Epub 2018 Aug 16. PMID: 29851073.
In vitro protocol:
Kanatsu K, Hori Y, Ebinuma I, Chiu YW, Tomita T. Retrograde transport of γ-secretase from endosomes to the trans-Golgi network regulates Aβ42 production. J Neurochem. 2018 Oct;147(1):110-123. doi: 10.1111/jnc.14477. Epub 2018 Aug 16. PMID: 29851073.
In vivo protocol:
TBD
1: Mecozzi VJ, Berman DE, Simoes S, Vetanovetz C, Awal MR, Patel VM, Schneider RT, Petsko GA, Ringe D, Small SA. Pharmacological chaperones stabilize retromer to limit APP processing. Nat Chem Biol. 2014 Jun;10(6):443-9. doi: 10.1038/nchembio.1508. Epub 2014 Apr 20. PubMed PMID: 24747528.