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236005

Sigma-Aldrich

COX-1 Inhibitor, FR122047

The COX-1 Inhibitor, FR122047, also referenced under CAS 130717-51-0, controls the biological activity of COX-1. This small molecule/inhibitor is primarily used for Cell Signaling applications.

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Synonym(s):
COX-1 Inhibitor, FR122047, FR 122047, 1-[(4,5-Bis(4-methoxyphenyl-2-thiazoyl)carbonyl]-4-methylpiperazine, Hydrochloride, 4,5-Bis(4-methoxyphenyl-2-[(1-methylpiperazin-4-yl)carbonyl]thiazole, Hydrochloride
Empirical Formula (Hill Notation):
C23H25N3O3S · xHCl
CAS Number:
Molecular Weight:
423.53 (free base basis)

Quality Level

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

pale yellow

solubility

1 M HCl: 2 mg/mL
water: 4 mg/mL
DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C23H25N3O3S.ClH/c1-25-12-14-26(15-13-25)23(27)22-24-20(16-4-8-18(28-2)9-5-16)21(30-22)17-6-10-19(29-3)11-7-17;/h4-11H,12-15H2,1-3H3;1H

InChI key

YWMAVHIKOAOSFM-UHFFFAOYSA-N

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236015553014124030
COX-1 Inhibitor, FR122047 The COX-1 Inhibitor, FR122047, also referenced under CAS 130717-51-0, controls the biological activity of COX-1. This small molecule/inhibitor is primarily used for Cell Signaling applications.

236005

COX-1 Inhibitor, FR122047

COX-2 Inhibitor V, FK3311 The COX-2 Inhibitor V, FK3311, also referenced under CAS 116686-15-8, controls the biological activity of COX-2. This small molecule/inhibitor is primarily used for Cell Signaling applications.

236015

COX-2 Inhibitor V, FK3311

Raf Kinase Inhibitor IV The Raf Kinase Inhibitor IV, also referenced under CAS 303727-31-3, controls the biological activity of Raf Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

553014

Raf Kinase Inhibitor IV

form

solid

form

solid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light, desiccated (hygroscopic)

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

General description

A cell-permeable trisubstituted thiazole compound that acts as a potent and selective inhibitor of COX-1 (IC50 = 28 nM and 65 µM for human recombinant COX-1 and COX-2, respectively). Displays ~2,300 fold greater selectivity towards inhibition of COX-1 over COX-2. Reported to be orally active and display analgesic, anti-platelet and anti-inflammatory properties.
A potent, cell-permeable, and selective inhibitor of COX-1 (IC50 = 28 nM; human recombinant COX-1). Does not significantly inhibit COX-2 (IC50 = 65 µM, human recombinant COX-2). Reported to be orally active and displays analgesic properties in chemical nociceptive animal models. Also reported to exhibit anti-inflammatory effects and suppress prostaglandin E2 and thromboxane 2 levels in collagen-induced arthritis in rats. Shown to be 100 times more potent than aspirin in inhibiting arachidonic acid- and collagen-induced human and guinea pig platelet aggregation.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
COX-1, COX-2
Product does not compete with ATP.
Reversible: no
Target IC50: 28 nM and 65 µM for human recombinant COX-1 and COX-2

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Ochi, T., and Goto, T. 2002. Br. J. Pharmacol.135, 782.
Ochi, T., et al. 2000. Eur. J. Pharmacol.391, 49.
Tanaka, A., et al. 1994. J. Med. Chem.37, 1189.
Dohi, M., et al. 1993. Eur. J. Pharmacol.243, 179.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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