2. Others Neuronal Signaling
  3. Drug Derivative Amyloid-β Beta-secretase
  4. TPT-260 Dihydrochloride

TPT-260 Dihydrochloride  (Synonyms: NSC55712; TPU-260 Dihydrochloride)

Cat. No.: HY-13769A Purity: 98.0%
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TPT-260 Dihydrochloride (NSC55712), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 Dihydrochloride increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 Dihydrochloride inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 Dihydrochloride improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 Dihydrochloride exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 Dihydrochloride can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease.

For research use only. We do not sell to patients.

TPT-260 Dihydrochloride

TPT-260 Dihydrochloride Chemical Structure

CAS No. : 2076-91-7

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Based on 2 publication(s) in Google Scholar

Other Forms of TPT-260 Dihydrochloride:

TPT-260 Dihydrochloride Related Antibodies

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2 Publications Citing Use of MCE TPT-260 Dihydrochloride

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Description

TPT-260 Dihydrochloride (NSC55712), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 Dihydrochloride increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 Dihydrochloride inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 Dihydrochloride improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 Dihydrochloride exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 Dihydrochloride can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease[1][2][3][4].

In Vitro

TPT-260 (10 μM) Dihydrochloride improves Occludin recycling and epithelial barrier function in Caco-2 cells but has no effect on VMP1-knockdown Caco-2 cells, indicating VMP1 is required for the Target Reagent's activity[1].
TPT-260 (5-20 μM) Dihydrochloride has no cytotoxic effect on primary mouse microglia, as measured by cell viability and LDH release assays[2].
TPT-260 (5-20 μM) Dihydrochloride protects primary mouse microglia from LPS (HY-D1056)/Nigericin (HY-127019)-induced cytotoxicity, as shown by restored cell viability and reduced LDH release[2].
TPT-260 (5-20 μM) Dihydrochloride inhibits LPS/Nigericin-induced inflammasome formation in primary mouse microglia, as measured by reduced ASC speck formation[2].
TPT-260 (5-20 μM) Dihydrochloride inhibits LPS/Nigericin-induced nuclear translocation of NF-κB p65 in primary mouse microglia, as measured by reduced nuclear p65 fluorescence intensity[2].
TPT-260 (5-20 μM) Dihydrochloride inhibits LPS (HY-D1056)/Nigericin (HY-127019)-induced upregulation of pro-inflammatory gene expression (Nlrp3, Tnfa, Il1b) in primary mouse microglia[2].
TPT-260 (5-20 μM) Dihydrochloride attenuates LPS/Nigericin-induced activation of the TLR4-IKKβ-NF-κB pathway in primary mouse microglia, as shown by reduced levels of pathway-related proteins and pro-inflammatory IL-1β[2].
TPT-260 (5 μM; 48 h) Dihydrochloride increases plasma membrane expression of NHE3 in Caco-2/bbe cells, raising surface NHE3 to 142.4% of control[3].
TPT-260 (5 μM; 48 h) Dihydrochloride increases levels of core retromer proteins VPS35 and VPS26 in Caco-2/bbe cells, and prevents the Cholera toxin (CT)-induced reduction in these retromer proteins when given either concurrently with CT or prior to CT exposure[3].
TPT-260 (5 μM; 48 h) Dihydrochloride increases plasma membrane expression of NHE3 in polarized Caco-2/bbe-HA-NHE3 cells, and reverses the CT-induced reduction in NHE3 surface expression when given either concurrently with CT or prior to CT exposure[3].
TPT-260 (5 μM; 48 h) Dihydrochloride partially reduces forskolin-induced fluid secretion in 3D human duodenal enteroids by stimulating NHE3-mediated fluid absorption[3].
TPT-260 Dihydrochloride (R55) binds to retromer complex with a Kd of ~5 μM[4].
TPT-260 Dihydrochloride (48 h) increases Vps35 levels with an EC50 of ~3.3 μM in primary hippocampal neurons[4].
TPT-260 Dihydrochloride (48 h) significantly reduces the levels of both endogenous Aβ40 and Aβ42 in hippocampal neurons[4].
TPT-260 Dihydrochloride inhibits Aβ levels with an IC50 of ~12 μM in hippocampal neurons[4].
TPT-260 Dihydrochloride significantly reduces the levels of both endogenous β-CTF and sAPPβ, and increases sAPPα levels in hippocampal neurons[4].

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

TPT-260 Dihydrochloride Related Antibodies

Western Blot Analysis[3]

Cell Line: Caco-2/bbe cells
Concentration: 5 μM
Incubation Time: 48 h
Result: Increased amounts of VPS35 to 125% of control and VPS26 to 129% of control when used alone.
Prevented the CT-induced reduction in VPS35 and VPS26 levels, maintaining them at levels similar to untreated controls when given concurrently with CT or before CT.
In Vivo

TPT-260 (5 mg/kg; i.p.; single dose 24 hours prior to MCAO surgery) Dihydrochloride significantly reduces brain infarct volume, lowers neuroinflammatory marker levels, and improves neurological function in ischemic stroke model mice by inhibiting NF-κB signaling and M1 microglial activation[2].

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

Animal Model: C57BL/6 (2-month-old) bearing middle cerebral artery occlusion (MCAO) surgery[2]
Dosage: 5 mg/kg
Administration: i.p.; single dose (24 hours prior to MCAO surgery)
Result: Significantly improved Bederson score (neurological function) in MCAO mice.
Significantly reduced brain infarct volume on the affected side.
Significantly suppressed brain tissue levels of pro-inflammatory factors IL-1β and TNF-α compared to untreated MCAO mice.
Molecular Weight

333.32

Formula

C8H14Cl2N4S3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC(SCC1=CC=C(CSC(N)=N)S1)=N.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (300.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.33 mg/mL (99.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0001 mL 15.0006 mL 30.0012 mL
5 mM 0.6000 mL 3.0001 mL 6.0002 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.0001 mL 15.0006 mL 30.0012 mL 75.0030 mL
5 mM 0.6000 mL 3.0001 mL 6.0002 mL 15.0006 mL
10 mM 0.3000 mL 1.5001 mL 3.0001 mL 7.5003 mL
15 mM 0.2000 mL 1.0000 mL 2.0001 mL 5.0002 mL
20 mM 0.1500 mL 0.7500 mL 1.5001 mL 3.7501 mL
25 mM 0.1200 mL 0.6000 mL 1.2000 mL 3.0001 mL
30 mM 0.1000 mL 0.5000 mL 1.0000 mL 2.5001 mL
40 mM 0.0750 mL 0.3750 mL 0.7500 mL 1.8751 mL
50 mM 0.0600 mL 0.3000 mL 0.6000 mL 1.5001 mL
60 mM 0.0500 mL 0.2500 mL 0.5000 mL 1.2500 mL
80 mM 0.0375 mL 0.1875 mL 0.3750 mL 0.9375 mL
DMSO 100 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7500 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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TPT-260 Dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

TPT-2602076-91-7NSC55712TPU-260TPT260TPT 260NSC 55712NSC-55712TPU260TPU 260Drug DerivativeAmyloid-βBeta-secretaseDrug derivativeβ-amyloid peptideAβAbetaBACEβ-SecretaseNLRP3 inflammasomeprimary microgliaTLR4IKKβischemic strokeCaco-2 cellsOccludinretromer complexNF-κB p65inflammatory bowel diseaseInhibitorinhibitorinhibit

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