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PF-4693627

Katalog-Nr.GC18700

PF-4693627 ist ein potenter, selektiver und oral bioverfÜgbarer mikrosomaler Prostaglandin-E-Synthase-1 (mPGES-1)-Inhibitor (IC50=3 nM) zur Behandlung von EntzÜndungen, die durch Osteoarthritis (OA) und rheumatoide Arthritis (RA) verursacht werden.

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PF-4693627 Chemische Struktur

Cas No.: 1312815-93-2

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500μg
52,00 $
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1mg
95,00 $
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5mg
449,00 $
Auf Lager
10mg
846,00 $
Auf Lager

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Sample solution is provided at 25 µL, 10mM.

Description of PF-4693627

PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1; IC50 = 3 nM). It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation.

Chemical Properties of PF-4693627

Cas No. 1312815-93-2 SDF
Chemical Name 1-[5-chloro-6-(4-chlorophenyl)-2-benzoxazolyl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-4-piperidinecarboxamide
Canonical SMILES ClC1=CC=C(C2=CC(OC(N3CCC(C(N[C@@H]4C[C@@H](CO)CCC4)=O)CC3)=N5)=C5C=C2Cl)C=C1
Formula C26H29Cl2N3O3 M.Wt 502.4
Löslichkeit DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: 5 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of PF-4693627

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1 mg 5 mg 10 mg
1 mM 1.9904 mL 9.9522 mL 19.9045 mL
5 mM 0.3981 mL 1.9904 mL 3.9809 mL
10 mM 0.199 mL 0.9952 mL 1.9904 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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