2. Immunology/Inflammation
  3. PGE synthase
  4. PF-4693627

PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).

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

PF-4693627 Chemical Structure

PF-4693627 Chemical Structure

CAS No. : 1312815-93-2

Size Price Stock Quantity
5 mg USD 512 In-stock
10 mg USD 820 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

PF-4693627 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA)[1].

IC50 & Target

IC50: 3 nM (mPGES-1)[1]
In Vitro

PF-4693627 also inhibits mPGES-1 with IC50s of 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively[1].
PF-4693627 shows high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC50=109 nM)[1].

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

PF-4693627 Related Antibodies
In Vivo

PF-4693627 (10 mg/kg; orally) inhibits 63% of PGE2 production relative to vehicle control in Guinea pig carrageenan stimulated air pouch model[1].
PF-4693627 (1.0 mg/kg; i.v.) shows good bioavailability (59%) and modest half life (t1/2=3.7 h) in Sprague-Dawley rats[1].

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

Animal Model: Guinea pig with carrageenan stimulated air pouch inflammation model[1]
Dosage: 10 mg/kg
Administration: Administered orally
Result: 63% PGE2 inhibition.
Animal Model: Sprague-Dawley rats[1].
Dosage: 1.0 mg/kg (Pharmacokinetic Analysis)
Administration: Administered i.v.
Result: Clearance (CL), volume of distribution (Vdss), t1/2, mean residence time (MRT) and bioavailability (F) is 12 mL/min/kg, 3.0 L/kg, 3.7 h, 4.42 h, 59%, respectively.
Molecular Weight

502.43

Formula

C26H29Cl2N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1CCN(C2=NC3=CC(Cl)=C(C4=CC=C(Cl)C=C4)C=C3O2)CC1)N[C@@H]5C[C@@H](CO)CCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (199.03 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 1.9903 mL 9.9516 mL 19.9033 mL
5 mM 0.3981 mL 1.9903 mL 3.9807 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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 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
Purity & Documentation

Purity: 99.63%

COA (245 KB) HNMR (148 KB) RP-HPLC (169 KB) LCMS (233 KB)

Handling Instructions (2659 KB)
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. 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
DMSO 1 mM 1.9903 mL 9.9516 mL 19.9033 mL 49.7582 mL
5 mM 0.3981 mL 1.9903 mL 3.9807 mL 9.9516 mL
10 mM 0.1990 mL 0.9952 mL 1.9903 mL 4.9758 mL
15 mM 0.1327 mL 0.6634 mL 1.3269 mL 3.3172 mL
20 mM 0.0995 mL 0.4976 mL 0.9952 mL 2.4879 mL
25 mM 0.0796 mL 0.3981 mL 0.7961 mL 1.9903 mL
30 mM 0.0663 mL 0.3317 mL 0.6634 mL 1.6586 mL
40 mM 0.0498 mL 0.2488 mL 0.4976 mL 1.2440 mL
50 mM 0.0398 mL 0.1990 mL 0.3981 mL 0.9952 mL
60 mM 0.0332 mL 0.1659 mL 0.3317 mL 0.8293 mL
80 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6220 mL
100 mM 0.0199 mL 0.0995 mL 0.1990 mL 0.4976 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PF-4693627 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-46936271312815-93-2PF4693627PF 4693627PGE synthaseProstaglandin E synthasemPGES-1orallybioavailableinflammationosteoarthritisrheumatoidarthritisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PF-4693627
Cat. No.:
HY-125415
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.