马立马司他 T6885

Product Introduction
Bioactivity


英文名: Marimastat

描述: Marimastat (BB2516) 是一种血管生成和转移抑制剂，限制血管的生长和生成。它是一种广谱的，具有口服活性的MMPs 抑制剂，有效抑制 MMP-9 , MMP-1, MMP-2, MMP-14, MMP-7，用于癌症的研究。

激酶实验: Compounds 1, 2, 7-9 and 11-16 are pre-incubated with MMP-1 or MMP-3 (10 nM) at different concentrations (0-10 μM) in a mixture of Tris-HCl (50 mM, pH 7.5), NaCl (150 mM), CaCl2 (10 mM), NaN3 (0.02%) and Brij-35 (0.05%) for 1 hour at 37°C. Residual activity is measured using the fluorogenic MMP substrate (2 μM) by fluorescence increase (emission at 393 nm and excitation at 325 nm) on a fluorescence plate reader. The data are fitted to the tight binding inhibitor equation: v=[(E-I-k+[(E-I-k)2+4Ek]1/2)/(2E)], where v is the velocity of the reaction, E is the enzyme concentration, I is the initial inhibitor concentration, and k is the apparent inhibition constant, using the software Prism.

体外活性: Marimastat (BB-2516) is a broad-spectrum MMPI with an enzyme inhibitory spectrum very similar to batimastat. [1] Marimastat inhibits CD30 shedding in Karpas 299 cells with an IC50 of 1 microM [2] and also inhibits LPS-induced soluble TNF-alpha production in a dose-dependent manner. The enzyme, tumor necrosis factor alpha convertase (TACE), reported to be closely related to matrix metalloproteinases, is responsible for the processing of pro-TNFalpha to TNFalpha and is specifically inhibited by Marimastat with an IC50 of 3.8 nM.[3]

体内活性: Marimastat has a favorable pharmacokinetic profile in humans, as it is almost completely absorbed after oral administration, with a high and predictable bioavailability and a half-life of approximately 15 hr (justifying twice a day dosing), making it a much more palatable treatment option for Clinicalal trials than batimastat. Marimastat is rapidly metabolized in rodents, undergoing a very high first-pass effect, making testing of marimastat in rodents difficult, as sustained plasma concentrations in this species are difficult to obtain. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 33.1 mg/mL (100 mM)


关键字: BB-2516 | KB-R 8898 | TA 2516 | inhibit | TA-2516 | Inhibitor | Marimastat | BB 2516 | KB-R-8898 | Matrix metalloproteinases | MMP

相关产品: JG26 | ethyl rosmarinate | CM-352 | TAPI-1 trifluoroacetate (163847-77-6(free base)) | Bacoside A | Doxycycline hydrochloride | Luteolin 7-O-glucuronide | MMP-9-IN-6 | Stigmasterol | NSC 405020

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Clinical Compound Library | Anti-Lung Cancer Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Orally Active Compound Library | Target-Focused Phenotypic Screening Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途