S-methyl-KE-298 (M-2)
(Synonyms: M-2) 目录号 : GC31734
S-methyl-KE-298 (M-2) 是 KE-298 的活性代谢物。
Cas No.:143584-75-2
Sample solution is provided at 25 µL, 10mM.
S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.
S-methyl-KE-298 is a methyl conjugate of deacetyl-KE-298 is plasma[1]. In vitro protein binding of KE-298 and its plasma metabolites, deacetyl-KE-298 (M-1) and S-methyl-KE-298 (M-2), is high in rat (>97%), dog (>89%) and human plasma (>99%), respectively[2]. KE-298 blocks this IL-1β-induced pro-MMP-2 activation and MT1-MMP expression, but does not affect IL-1β-induced tissue inhibitor of metalloproteinase-2 (TIMP-2) secretion from rheumatoid synovial cells. KE-298 inhibits MMP-1 production from rheumatoid arthritis (RA) synovial cells by affecting a transcription factor, AP-1. KE-298 inhibits the basal levels of MT1-MMP expression of unstimulated rheumatoid synovial cells[3].
[1]. Yoshida H, et al. Identification of metabolites of KE-298, a new antirheumatic drug, and its physiological properties in rats. Biol Pharm Bull. 1996 Mar;19(3):424-9. [2]. Endo H, et al. Stereoselectivity and species difference in plasma protein binding of KE-298 and its metabolites. Biol Pharm Bull. 2001 Jul;24(7):800-5. [3]. Honda S, et al. Expression of membrane-type 1 matrix metalloproteinase in rheumatoid synovial cells. Clin Exp Immunol. 2001 Oct;126(1):131-6.
Cas No. | 143584-75-2 | SDF | |
别名 | M-2 | ||
Canonical SMILES | CSCC(C(O)=O)CC(C1=CC=C(C)C=C1)=O | ||
分子式 | C13H16O3S | 分子量 | 252.33 |
溶解度 | DMSO : 100 mg/mL (396.31 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 3.9631 mL | 19.8153 mL | 39.6306 mL |
5 mM | 0.7926 mL | 3.9631 mL | 7.9261 mL |
10 mM | 0.3963 mL | 1.9815 mL | 3.9631 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00%
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