FR 122047 hydrochlorideA highly selective Cox-1 inhibitor

FR 122047 hydrochloride (CAS 130717-51-0)

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Synonym: 1-[[4,5-bis(4-methoxyphenyl)-2-thiazolyl]carbonyl]-4-methyl-piperazine
Application: A highly selective Cox-1 inhibitor
CAS Number: 130717-51-0
Molecular Weight: 459.99
Molecular Formula: C23H25N3O3S•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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FR 122047 hydrochloride is the hydrochloride salt preparation of FR 122047 and is a Cox-1 (cyclooxygenase-1) and Cox-2 inhibitor. FR 122047 is highly selective for Cox-1 (IC50 of 0.028 μM) over Cox-2 (IC50 of 65 μM). This compound has been shown to inhibit arachidonic acid (sc-200770)-induced guinea-pig platelet aggregation in vitro. FR 122047 also displays the capacity to inhibit malondialdehyde (MDA) synthesis and cause vasodilation in vitro. Further studies suggest that FR 122047 is also capable of suppressing prostaglandin E2 (PGE2, sc-201225) and Thromboxane B2 (TXB2, sc-201452) levels which results in an anti-inflammatory effect.


References

1. Dohi, M., et al. 1993. Eur. J. Pharmacol. 243: 179-184. PMID: 8276067
2. Tanaka, A., et al. 1994. J. Med. Chem. 37: 1189-1199. PMID: 8164261
3. Ochi, T., et al. 2000. Eur. J. Pharmacol. 391: 49-54. PMID: 10720634
4. Ochi, T. and Goto, T. 2002. Br. J. Pharmacol. 135: 782-788. PMID: 11834626

Physical State :
Solid
Solubility :
Soluble in DMSO, water (10 mM), and methylene chloride (50 mg/ml).
Storage :
Store at -20° C
Boiling Point :
562.7° C at 760 mmHg (Predicted)
Refractive Index :
n20D ~1.60 (Predicted)
IC50 :
Cox-1: IC50 = 28 nM (human); Cox-2: IC50 = 65 µM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
196840
MDL Number :
MFCD00925604
SMILES :
CN1CCN(CC1)C(=O)C2=NC(=C(S2)C3=CC=C(C=C3)OC)C4=CC=C(C=C4)OC.Cl

Download SDS (MSDS)

Certificate of Analysis

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