Marimastat NEW
| Price | $54 | $85 | $129 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-16 |
Product Details
| Product Name: Marimastat | CAS No.: 154039-60-8 |
| Purity: 98.11% | Supply Ability: 10g |
| Release date: 2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | Marimastat |
| 描述 | Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM). |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 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] |
| 體內(nèi)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] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 33.1 mg/mL (100 mM) |
| 關(guān)鍵字 | BB-2516 | KB-R 8898 | TA 2516 | inhibit | TA-2516 | Inhibitor | Marimastat | BB 2516 | KB-R-8898 | Matrix metalloproteinases | MMP |
| 相關(guān)產(chǎn)品 | Stigmasterol | Ethyl gallate | Doxycycline (hyclate) | Chondroitin sulfate | Astragaloside IV | Doxycycline | Edaravone | Glucosamine | Triolein | Glucosamine sulfate |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | 抗心血管疾病化合物庫(kù) | 抗纖維化化合物庫(kù) | 已知活性化合物庫(kù) | 人代謝物化合物庫(kù) | 抗癌活性化合物庫(kù) | 抗癌藥物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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