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PF-1355 (Synonyms: PF-06281355)

Cat. No.: HY-100873 Purity: 99.51%
Handling Instructions

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

PF-1355 Chemical Structure

CAS No. : 1435467-38-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 552 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1020 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

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].

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].

Solvent & Solubility
In Vitro: 

DMSO : 8.75 mg/mL (27.23 mM; Need ultrasonic and warming)

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
*Please refer to the solubility information to select the appropriate solvent.
References
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
Molecular Weight

321.35

Formula

C₁₄H₁₅N₃O₄S

CAS No.

1435467-38-1

SMILES

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

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

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Product Name:
PF-1355
Cat. No.:
HY-100873
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PF-1355

Cat. No.: HY-100873