236005

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.

• 동의어(들): 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
• 실험식(Hill 표기법): C₂₃H₂₅N₃O₃S · xHCl
• CAS Number: 130717-51-0
• Molecular Weight: 423.53 (free base basis)
• UNSPSC 코드: 51111800
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; desiccated (hygroscopic); protect from light
• 색상: pale yellow
• solubility: 1 M HCl: 2 mg/mL; water: 4 mg/mL; DMSO: 5 mg/mL
• 배송 상태: ambient
• 저장 온도: 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

설명

일반 설명

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.

생화학적/생리학적 작용

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable