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FR 122047 hydrochloride

Cyclooxygenase (COX-1) inhibitor CAS# 130717-51-0

FR 122047 hydrochloride

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Chemical structure

FR 122047 hydrochloride

3D structure

Chemical Properties of FR 122047 hydrochloride

Cas No. 130717-51-0 SDF Download SDF
PubChem ID 196840 Appearance Powder
Formula C23H26ClN3O3S M.Wt 459.99
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in water
Chemical Name [4,5-bis(4-methoxyphenyl)-1,3-thiazol-2-yl]-(4-methylpiperazin-1-yl)methanone;hydrochloride
SMILES CN1CCN(CC1)C(=O)C2=NC(=C(S2)C3=CC=C(C=C3)OC)C4=CC=C(C=C4)OC.Cl
Standard InChIKey YWMAVHIKOAOSFM-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of FR 122047 hydrochloride

DescriptionSelective 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.

FR 122047 hydrochloride Dilution Calculator

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FR 122047 hydrochloride Molarity Calculator

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Preparing Stock Solutions of FR 122047 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.174 mL 10.8698 mL 21.7396 mL 43.4792 mL 54.349 mL
5 mM 0.4348 mL 2.174 mL 4.3479 mL 8.6958 mL 10.8698 mL
10 mM 0.2174 mL 1.087 mL 2.174 mL 4.3479 mL 5.4349 mL
50 mM 0.0435 mL 0.2174 mL 0.4348 mL 0.8696 mL 1.087 mL
100 mM 0.0217 mL 0.1087 mL 0.2174 mL 0.4348 mL 0.5435 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on FR 122047 hydrochloride

Differential effect of FR122047, a selective cyclo-oxygenase-1 inhibitor, in rat chronic models of arthritis.[Pubmed:11834626]

Br J Pharmacol. 2002 Feb;135(3):782-8.

We investigated the effects of FR122047 (1-[(4,5-bis(4-methoxyphenyl)-2-thiazoyl)carbonyl]-4-methylpiperazine hydrochloride), a selective cyclo-oxygenase (COX)-1 inhibitor, in rat type II collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA). Using an ex vivo rat whole blood assay, FR122047 (0.032 - 3.2 mg kg(-1)) inhibited COX-1-derived thromboxane (TX) B(2) production with ED(50) value of 0.059 mg kg(-1), indicating that it was orally active, but did not inhibit lipopolysaccharide-induced prostaglandin (PG) E(2) production derived by COX-2. Oral administration of FR122047 showed a dose-dependent anti-inflammatory effect in rat CIA with ED(50) value of 0.56 mg kg(-1). This drug also dose dependently suppressed the levels of PGE(2) and TXB(2) in CIA rat paws with ED(50) values of 0.24 and 0.13 mg kg(-1), respectively. FR122047 had no effect in rat AIA model. In contrast, indomethacin, a non-selective COX inhibitor, was anti-inflammatory and reduced the formation of PGs in AIA rat paws. Unlike indomethacin, chronic treatment of FR122047 did not damage the stomach mucosa in CIA rats. These results demonstrate that COX-1 contributes to the oedema and the formation of PGE(2) and TXB(2) in rat CIA model, but not in rat AIA model. We conclude that FR122047 has an orally active and anti-inflammatory effect mediated by inhibition of PGE(2) and TXB(2) produced by COX-1 at a site of inflammation induced by type II collagen and it may be a useful tool for studying the involvement of COX-1 in various in vivo models of inflammation.

The analgesic effect profile of FR122047, a selective cyclooxygenase-1 inhibitor, in chemical nociceptive models.[Pubmed:10720634]

Eur J Pharmacol. 2000 Mar 10;391(1-2):49-54.

The pharmacological profile of the analgesic agent, 1-[(4, 5-bis(4-methoxyphenyl)-2-thiazoyl)carbonyl]-4-methylpiperazine hydrochloride (FR122047), was investigated. In recombinant human cyclooxygenase enzyme assays, the inhibition of prostaglandin E(2) formation by FR122047 was 2300 times more selective for cyclooxygenase-1 than cyclooxygenase-2. Oral administration of FR122047 (3.2-100 mg/kg) dose dependently reduced the phase 2 response (10-60 min) of the formalin test in rats. This effect was 3 times less potent than that of indomethacin. FR122047 (1-32 mg/kg; p. o.) showed a dose-dependent analgesic effect against the acetic acid-induced writhing response in mice. Furthermore, FR122047 (0. 01-10 mg/kg, p.o.) inhibited the increase in 6-keto prostaglandin F(1alpha) level in acetic acid-injected mouse peritoneal cavity. However, a selective cyclooxygenase-2 inhibitor, NS-398, had no effect in these cyclooxygenase-1 sensitive pain models. These results suggest that FR122047, a selective cyclooxygenase-1 inhibitor, shows an analgesic effect in chemical nociceptive models and may be a useful analgesic agent.

Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.[Pubmed:8164261]

J Med Chem. 1994 Apr 15;37(8):1189-99.

The syntheses, biological evaluations, and structure-activity relationships of a series of 4,5-bis-(4-methoxyphenyl)-2-substituted-thiazoles as potent antiplatelet agents with vasodilatory activity are described. 2-Guanidino-4,5-bis(4-methoxyphenyl)thiazole (3), designed from two parent compounds (itazigrel and timegadine), showed inhibitory activity of malondialdehyde (MDA, IC50 = 31 microM) production which is formed from the cyclooxygenase (CO)-catalyzed oxygenation of arachidonic acid in the synthesis of prostanoids in platelets, with vasodilatory activity (ED50 = 2.0 microM). Further structure-activity relationship studies on 3 culminated in the preparation of 4,5-bis(4-methoxyphenyl)-2-[(1-methylpiperazin-4-yl)carbonyl]thiaz ole (10a, FR122047) which exhibited potent inhibitory activity on MDA synthesis in vitro (IC50 = 0.088 microM) and platelet aggregation in guinea pigs ex vivo (100% inhibition even 6 h after 1.0 mg/kg administration) with vasodilatory activity in vitro (ED50 = 6.2 microM). Moreover, 10a demonstrated no ulcerogenesis effect in rats even at 100 mg/kg dosage (safety margin in rats is more than 70 while that of aspirin is only 1.2) in spite of its potent CO inhibition (IC50 = 0.43 microM14), while the use of aspirin, a CO inhibitor and the most popular thromboembolic drug, is restricted by the side effect. Pharmacokinetic studies on 10a have revealed that 10a is detectable in platelet-rich plasma but not in platelet-poor plasma 1 day after oral administration, which indicates that 10a tends to be localized in platelets. This property could be responsible for its low toxicity and reduction of side effects in clinical studies.

The anti-platelet actions of FR122047, a novel cyclooxygenase inhibitor.[Pubmed:8276067]

Eur J Pharmacol. 1993 Oct 19;243(2):179-84.

The anti-platelet actions of 1-[(4,5-bis(4-methoxyphenyl)-2- thiazoyl)carbonyl]-4-methylpiperazine hydrochloride (FR122047) were investigated in vitro and in vivo. FR122047 was 100 times more potent than aspirin against arachidonic acid- and collagen-induced human and guinea-pig platelet aggregation in vitro. Its actions on platelets were a result of cyclooxygenase inhibition. The single oral dose of FR122047 inhibited arachidonic acid- and collagen-induced aggregation with an ED50 of 280 micrograms/kg and 530 micrograms/kg, respectively, in guinea-pigs. The anti-platelet action was augmented 5-10 times by repeated administration for 4 days. At 1 mg/kg the inhibitory actions were prolonged for 48 h and the drug concentration was < 0.1 ng/ml in platelet-poor plasma at 24 h and 0.282 ng/ml in platelet-rich plasma at 48 h. The safety margin in rats (minimum ulcerogenic dose/ED50 for anti-platelet aggregation) of FR122047 was more than 70, while that of aspirin was only 1.2. These results indicate that FR122047 is concentrated in platelets and may be a useful anti-platelet agent.

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