2. Apoptosis Metabolic Enzyme/Protease
  3. Glutathione Peroxidase
  4. PF-06282999

PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.

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

PF-06282999 Chemical Structure

PF-06282999 Chemical Structure

CAS No. : 1435467-37-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

PF-06282999 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.

In Vitro

PF-06282999 (Compound 8) is a potent and selective myeloperoxidase inhibitor. The estimated EC50 for total PF-06282999 concentration in plasma is 3.8 μM, which corresponds well with the IC50 value obtained in the human whole blood assay of 1.9 μM[2].

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

PF-06282999 Related Antibodies
In Vivo

PF-06282999 is moderately bound to plasma proteins across preclinical species and humans. The blood/plasma ratios for PF-06282999 are 1.1, 1.1, 0.91, 1.2, and 0.94 in mice, rats, dogs, monkeys, and humans, respectively, suggesting that PF-06282999 is equally distributed into plasma and red blood cells[1]. The in vivo pharmacokinetics of PF-06282999 are examined in greater detail in mice, rats, dogs, and monkeys, wherein it is demonstrated to have low CLp in mice (10.1 mL/min/kg), dogs (3.39 mL/min/kg), monkeys (10.3 mL/min/kg) and moderate CLp in rats (41.8 mL/min/kg). The terminal plasma elimination half-lives (t1/2) range from 0.75 to 3.3 h in the four species. Approximately 26-32% of the iv dose of PF-06282999 is excreted in the unchanged form in rat, dog, and monkey urine, wherein it is also shown that it is well distributed with steady state distribution volumes (Vdss) ranging from 0.5-2.1 L/kg in mice, rats, dogs, and monkeys. Following oral administration, PF-06282999 is rapidly (Tmax=0.78-1.70 h) and well absorbed in mice, rats, dogs, and monkeys with oral bioavailability values of 100%, 86%, 75%, and 76%, respectively[2].

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

325.77

Formula

C13H12ClN3O3S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N)CN(C(C1=CC(Cl)=CC=C1OC)=C2)C(NC2=O)=S
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (306.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0697 mL 15.3483 mL 30.6965 mL
5 mM 0.6139 mL 3.0697 mL 6.1393 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (7.67 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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 (7.67 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.02%

SDS (393 KB)

COA (256 KB) LCMS (104 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[2]

Test compound is incubated with human whole blood stimulated with bacterial LPS for 4 h, followed by capture of MPO on immobilized anti-MPO antibody coated plates. The captured MPO is washed and residual MPO activity is determined using Amplex Red and H2O2.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

In order to ascertain whether the advances noted in the in vitro and ex vivo assays for candidate thiouracil derivatives translated to effective irreversible inhibition of MPO in vivo, PF-06282999 is also advanced to an in vivo pharmacology study in cynomolgus monkeys using iv endotoxin (LPS) challenge, a classic model of inflammatory leukocyte activation with corresponding MPO activation demonstrated in various species including human. In this randomized crossover study, cynomolgus monkeys are orally administered either vehicle or PF-06282999 (5, 20, and 80 mg/kg) 1 h after iv administration of LPS. Blood is sampled throughout the study and heparinized plasma prepared for MPO activity measurements as well as determination of 8 plasma concentrations. Total MPO is captured using anti-MPO antibody coated plates, and following exchange of plasma for drug-free assay media, the residual activity of the captured MPO is measured using the peroxidation of Amplex Red. A mixed effect sigmoid model is applied to study the relationship between plasma exposure of PF-06282999 and the MPO capture activity at 2 h after dose and 3 h after LPS administration, which corresponds to the peak of MPO activity.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0697 mL 15.3483 mL 30.6965 mL 76.7413 mL
5 mM 0.6139 mL 3.0697 mL 6.1393 mL 15.3483 mL
10 mM 0.3070 mL 1.5348 mL 3.0697 mL 7.6741 mL
15 mM 0.2046 mL 1.0232 mL 2.0464 mL 5.1161 mL
20 mM 0.1535 mL 0.7674 mL 1.5348 mL 3.8371 mL
25 mM 0.1228 mL 0.6139 mL 1.2279 mL 3.0697 mL
30 mM 0.1023 mL 0.5116 mL 1.0232 mL 2.5580 mL
40 mM 0.0767 mL 0.3837 mL 0.7674 mL 1.9185 mL
50 mM 0.0614 mL 0.3070 mL 0.6139 mL 1.5348 mL
60 mM 0.0512 mL 0.2558 mL 0.5116 mL 1.2790 mL
80 mM 0.0384 mL 0.1919 mL 0.3837 mL 0.9593 mL
100 mM 0.0307 mL 0.1535 mL 0.3070 mL 0.7674 mL
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PF-06282999 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:

PF-062829991435467-37-0PF06282999PF 06282999Glutathione PeroxidaseInhibitorinhibitorinhibit

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