FR 122047 hydrochloride

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Cat.No. 1507 - FR 122047 hydrochloride | C23H25N3O3S.HCl | CAS No. 130717-51-0
Description: Cyclooxygenase (COX-1) inhibitor
Chemical Name: 1-[[4,5-bis(4-Methoxyphenyl)-2-thiazolyl]carbonyl]-4-methylpiperazine hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Literature

Biological Activity

Selective cyclooxygenase-1 (COX-1) inhibitor (IC50 values are 0.028 and 65 μM for COX-1 and COX-2 respectively). Antiplatelet, analgesic and anti-inflammatory following oral administration in vivo.

Technical Data

M. Wt 459.99
Formula C23H25N3O3S.HCl
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 130717-51-0
PubChem ID 196840
InChI Key YWMAVHIKOAOSFM-UHFFFAOYSA-N
Smiles Cl.COC1=CC=C(C=C1)C1=C(N=C(S1)C(=O)N1CCN(C)CC1)C1=CC=C(OC)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 2.3 5
DMSO 46 100
ethanol 11.5 25
water 4.6 10

Preparing Stock Solutions

The following data is based on the product molecular weight 459.99. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.17 mL 10.87 mL 21.74 mL
5 mM 0.43 mL 2.17 mL 4.35 mL
10 mM 0.22 mL 1.09 mL 2.17 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Dohi et al (1993) The anti-platelet actions of FR122047, a novel cyclooxygenase inhibitor. Eur.J.Pharmacol. 243 179 PMID: 8276067

Ochi et al (2000) The analgesic effect profile of FR122047, a selective cyclo-oxygenase-1 inhibitor, in chemical nociceptive models. Eur.J.Pharmacol. 391 49 PMID: 10720634

Ochi and Goto (2002) Differential effect of FR122047, a selective cyclo-oxygenase-1 inhibitor, in rat chronic models of arthritis. Br.J.Pharmacol. 135 782 PMID: 11834626

Tanaka et al (1994) Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles. J.Med.Chem. 37 1189 PMID: 8164261


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Keywords: Cyclooxygenase COX-1 inhibitors inhibits Oxygenases Oxidases FR122047 hydrochloride Cyclooxygenase

6 Citations for FR 122047 hydrochloride

Citations are publications that use Tocris products. Selected citations for FR 122047 hydrochloride include:

Tunaru et al (2016) Arachidonic acid metabolite 19(S)-HETE induces vasorelaxation and platelet inhibition by activating prostacyclin (IP) receptor. PLoS One 11 e0163633 PMID: 27662627

Lu et al (2013) Aspirin minimized the pro-metastasis effect of sorafenib and improved survival by up-regulating HTATIP2 in hepatocellular carcinoma. J Biol Chem 8 e65023 PMID: 23741443

Tunaru et al (2012) Castor oil induces laxation and uterus contraction via ricinoleic acid activating prostaglandin EP3 receptors. PLoS One 109 9179 PMID: 22615395

Chia et al (2011) Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice. BMC Pharmacol 11 10 PMID: 21955547

Passafaro et al (2011) Cholinergic Autoantibodies from Primary Sjögren's Syndrome Inhibit Mucin Production via Phospholipase C and Cyclooxygenase-2 In the Rat Submandibular Gland. J Virol 8 138 PMID: 22013477

Ray et al (2004) Cyclooxygenase-1 and -2 are required for production of infectious pseudorabies virus. Proc Natl Acad Sci U S A 78 12964 PMID: 15542648


Do you know of a great paper that uses FR 122047 hydrochloride from Tocris? If so please let us know.

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