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TES-1025 

Cat. No.: HY-111365 Purity: 98.12%
Handling Instructions

TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13±3 nM.

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

TES-1025 Chemical Structure

TES-1025 Chemical Structure

CAS No. : 1883602-21-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13±3 nM.

IC50 & Target

IC50: 13±3 nM (human ACMSD)[1]

In Vitro

TES-1025 is a low nanomolar human ACMSD inhibitor, which increases NAD+ levels in cellular systems[1].

In Vivo

TES-1025 is subjected to in vivo pharmacokinetic studies, following intravenous (IV) and oral (PO) dosings of male CD-1 mice. After the intravenous administration of 0.5 mg/kg, TES-1025 shows low blood clearance, with low volumes of distribution and half-lives (t1/2) of about 5.33 h, although after oral administration at 5 mg/kg, the blood concentration of TES-1025 is quantifiable for up to 8 h. A good systemic exposure is recorded for TES-1025, with a Cmax of 2570 ng/mL reaches at 2 h after dosing. The greater oral exposure of TES-1025 is further confirmed in the liver and kidneys with AUC0-8h of 19 200 h•ng/mL and 36 600 h•ng/mL, respectively[1].

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (260.80 mM; Need warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6080 mL 13.0399 mL 26.0797 mL
5 mM 0.5216 mL 2.6080 mL 5.2159 mL
10 mM 0.2608 mL 1.3040 mL 2.6080 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Recombinant hACMSD is expressed in Pichia pastoris and purified. Its enzyme activity is assayed by a coupled spectrophotometric assay. Briefly, in a pre-assay mixture, the ACMS substrate is generated from 10 μM 3-hydroxyanthranilic acid by recombinant 3-hydroxyanthranilate 3,4-dioxigenase from Ralstonia metallidurans. ACMS formation is monitored at 360 nm, and after the reaction is complete, an appropriate amount of ACMSD is added. Activity is calculated from the initial rate of the absorbance decrease subtracted from that of a control reaction mixture in the absence of ACMSD. The effects of the various compounds (e.g., TES-1025) on the enzyme activity are tested by adding the compounds to the assay mixture along with ACMSD. For the IC50 evaluations for each compound, a serial dilution from a stock solution prepared in DMSO is tested, maintaining a DMSO concentration in all the reaction mixtures of 1.0%. One unit is defined as the amount of enzyme that consume 1 μmol of ACMS per minute at 37°C[1].

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

Animal Administration
[1]

Mice[1]
Male CD-1 mice are used.The study is conducted in 3 phases. Phase 1: 18 mice receive an oral administration of TES-1025 at a target dose level of 5 mg/kg. Blood, brain and liver are collected at intervals up to 8 h after dose administration (n=3 animals per each time point). Phase 2: 3 mice receive each an intravenous administration of TES-1025 at a target dose of 0.5 mg/kg. Blood samples are collected from the lateral tail vein at intervals up to 24 h after dose administration. Phase 3: 3 mice receive a single intravenous administration of Elacridar (5 mg/kg) shortly before an oral administration of TES-1025 at a target dose of 5 mg/kg. Blood and brain samples are collected 0.5 h after dose administration. Brain, liver and kidney are collected from all animals of the study[1].

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

References
Molecular Weight

383.44

Formula

C₁₈H₁₃N₃O₃S₂

CAS No.

1883602-21-8

SMILES

O=C1C(C#N)=C(C2=CC=CS2)N=C(SCC3=CC=CC(CC(O)=O)=C3)N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.12%

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Product Name:
TES-1025
Cat. No.:
HY-111365
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TES-1025

Cat. No.: HY-111365