PF-1355 (Synonyms: PF-06281355)

Name: PF-1355
Brand: MedChemExpress
SKU: HY-100873
Rating: 5.0 (2 reviews)

Cat. No.: HY-100873 Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PF-1355 is a selective 2-thiouracil mechanism-based MPO inhibitor, used for treatment of vasculitic diseases.

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

PF-1355 Chemical Structure

CAS No. : 1435467-38-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 99	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 99	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE PF-1355

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

PF-1355 is a selective 2-thiouracil mechanism-based MPO inhibitor, used for treatment of vasculitic diseases.

In Vitro

In a dose-responsive fashion, PF-1355 inhibits MPO activity in phorbol ester-stimulated human neutrophils as measured by taurine chlorination (EC₅₀=1.47 μM) as well as lipopolysaccharide-treated human blood measuring residual MPO activity (EC₅₀=2.03 μM)^[1].

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

In Vivo

Oral administration of PF-1355 reduces plasma MPO activity, vascular edema, neutrophil recruitment, and elevates circulating cytokines. In a model of anti-glomerular basement membrane disease, formerly known as Goodpasture disease, albuminuria and chronic renal dysfunction are completely suppressed by PF-1355 treatment^[1].

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

Molecular Weight

321.35

Formula

C₁₄H₁₅N₃O₄S

CAS No.

1435467-38-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(N)CN(C(N1)=S)C(C2=CC(OC)=CC=C2OC)=CC1=O

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 : 50 mg/mL (155.59 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	3.1119 mL	15.5594 mL	31.1187 mL
5 mM	0.6224 mL	3.1119 mL	6.2237 mL
10 mM	0.3112 mL	1.5559 mL	3.1119 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.08 mg/mL (6.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.80%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (254 KB) HNMR (141 KB) LCMS (136 KB)

Handling Instructions (2659 KB)

References

[1]. Zheng W, et al. PF-1355, a mechanism-based myeloperoxidase inhibitor, prevents immune complex vasculitis and anti-glomerular basement membrane glomerulonephritis. J Pharmacol Exp Ther. 2015 May;353(2):288-98 [Content Brief]

Kinase Assay ^[1]	Plates are coated with the MPO capture antibody (1:200) overnight at 4°C, washed with PBS, and then nonspecific binding blocked with PBS/1% BSA. Plasma or peritoneal exudate samples are diluted 1:4 in PBS and 50 μL is added to triplicate wells for 1 hour at room temperature. Plates are washed three times with PBS containing 0.05% Tween, followed by PBS ishes. Assay buffer (50 μL containing 50 nM phosphate buffer, pH 7.4, containing 140 mM NaCl, 10 mM Na₂NO₂, 40 μM Amplex Red, and 10 μM H₂O₂) is added with kinetic reads and an excitation/emission wavelength of 530/580 nm on a fluorescence plate reader. Assay linearity is typically maintained for >300 seconds (R2 > 0.99) and Vmax represented by the change in relative fluorescence units divided by time to yield MPO activity. Active MPO is back-calculated using purified human MPO standard. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Animals receive an intraperitoneal injection of 4% thioglycollate broth in phosphate-buffered saline (PBS) for neutrophil recruitmen. Twenty hours later, PF-1355 or vehicle (1% hydroxypropyl methylcellulose, 0.5% 2-amino-2-hydroxymethyl-propane-1,3-diol, 0.5% hypromellose acetate succinate, pH 9.5) is administered p.o., followed by intraperitoneal administration of opsonized zymosan or saline. After 3 hours, the mice are euthanized and receive intraperitoneal injection of 2 mL cold PBS. Blood is collected and animals are shaken vigorously before the collection of peritoneal lavage. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zheng W, et al. PF-1355, a mechanism-based myeloperoxidase inhibitor, prevents immune complex vasculitis and anti-glomerular basement membrane glomerulonephritis. J Pharmacol Exp Ther. 2015 May;353(2):288-98 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1119 mL	15.5594 mL	31.1187 mL	77.7968 mL
	5 mM	0.6224 mL	3.1119 mL	6.2237 mL	15.5594 mL
	10 mM	0.3112 mL	1.5559 mL	3.1119 mL	7.7797 mL
	15 mM	0.2075 mL	1.0373 mL	2.0746 mL	5.1865 mL
	20 mM	0.1556 mL	0.7780 mL	1.5559 mL	3.8898 mL
	25 mM	0.1245 mL	0.6224 mL	1.2447 mL	3.1119 mL
	30 mM	0.1037 mL	0.5186 mL	1.0373 mL	2.5932 mL
	40 mM	0.0778 mL	0.3890 mL	0.7780 mL	1.9449 mL
	50 mM	0.0622 mL	0.3112 mL	0.6224 mL	1.5559 mL
	60 mM	0.0519 mL	0.2593 mL	0.5186 mL	1.2966 mL
	80 mM	0.0389 mL	0.1945 mL	0.3890 mL	0.9725 mL
	100 mM	0.0311 mL	0.1556 mL	0.3112 mL	0.7780 mL

PF-1355 Related Classifications

Cardiovascular Disease

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-13551435467-38-1PF-06281355PF1355PF 1355PF06281355PF 06281355Glutathione PeroxidaseInhibitorinhibitorinhibit

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PF-1355 (Synonyms: PF-06281355)

Customer Review

PF-1355 Related Antibodies

2 Publications Citing Use of MCE PF-1355

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

PF-1355 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PF-1355 Related Classifications

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