FR-188582

Cat. No.: HY-U00146 Purity: 99.12%: FAQs
Data Sheet SDS COA Handling Instructions

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FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC₅₀ value of 17 nM.

For research use only. We do not sell to patients.

FR-188582 Chemical Structure

CAS No. : 189699-82-9

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1 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
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Description

FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC₅₀ value of 17 nM.

IC₅₀ & Target^[1]

COX-2

17 nM (IC₅₀)

In Vitro

In a recombinant human cyclooxygenase (COX) enzyme activity, FR-188582 (FR188582) inhibits COX-2 with an IC₅₀ value of 17 nM, and the inhibition of prostaglandin (PG) E2 formation by FR188582 isover 6000 times more selective for COX-2 than COX-1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral administration of FR-188582 (0.01-3.2 mg/kg) reverses paw edema in adjuvant arthritic rats and shows a therapeutic effect in a dose-dependent manner with ED₅₀ values (95% C.L.) of 0.074 (0.00021-0.53) and 0.063 (0.0039-0.31) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively. The anti-inflammatory effect of FR-188582 (FR188582) is threefold more potent than that of Indomethacin with ED₅₀ values (95% C.L.) of 0.24 (0.047-1.8) and 0.20 (0.021-0.79) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

332.80

Formula

C₁₆H₁₃ClN₂O₂S

CAS No.

189699-82-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C1=CC=C(C2=CC(Cl)=NN2C3=CC=CC=C3)C=C1)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Purity: 99.12%

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Data Sheet (277 KB) SDS (251 KB)

COA (256 KB) LCMS (100 KB)

Handling Instructions (2659 KB)

References

[1]. Ochi T, et al. The anti-inflammatory effect of FR188582, a highly selective inhibitor of cyclooxygenase-2, with an ulcerogenic sparing effect in rats. Jpn J Pharmacol. 2001 Feb;85(2):175-82. [Content Brief]

Kinase Assay ^[1]	Human recombinant COX-1 and COX-2 are expressed in Chinese hamster ovary cells. The appropriate COX enzyme (1 μg for COX-1 and/or 3 μg for COX-2) is preincubated in 100 mM Tris-HCl buffer (pH 7.3) containing hematin (2 μM) and tryptophan (5 mM) with drugs (0.0001-100 μM) dissolved in 1% DMSO for 5 min at 37°C prior to the addition of Arachidonic acid (10 μM) for 5 min at 37°C. Reactions are terminated by the addition of 1N HCl, and PGE₂ production is measured by radioimmunoassay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Rats^[1] Female Lewis rats (140-180g) at the age of 8 weeks are used. Adjuvant arthritis is induced in female Lewis rats by intradermal injection into the plantar suface of the right hind paw of 0.5 mg of a suspension of heat-killed and dried Mycobacterium tuberculosis H37 RA in 0.05 mL of liquid Paraffin (day 0). The drugs, suspended and diluted on 0.5% methylcellulose, are given orally once a day therapeutically from day 15 to day 24 after adjuvant injection. Paw volume is measured before and 15,18,21,24 days after adjuvant injection with the Volume Meter TK-105, and edema is expressed as the increase in paw volume after adjuvant injection relative to the pre-injection value for each animal.The anti-inflammatory effect is expressed as the difference in paw edema compared with that of vehicle-treated adjuvant-control rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Ochi T, et al. The anti-inflammatory effect of FR188582, a highly selective inhibitor of cyclooxygenase-2, with an ulcerogenic sparing effect in rats. Jpn J Pharmacol. 2001 Feb;85(2):175-82. [Content Brief]

FR-188582 Related Classifications

Inflammation/Immunology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FR-188582189699-82-9FR188582FR 188582COXCyclooxygenaseInhibitorinhibitorinhibit

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