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Marimastat

Name: Marimastat
Brand: TargetMol
SKU: T6885
Price: 54 USD
Availability: InStock
Rating: 5 (10 reviews)

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).

Catalog No. T6885Cas No. 154039-60-8

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Purity:98.11%

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COA HNMR HPLC

Marimastat

Catalog No. T6885Cas No. 154039-60-8

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).

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Pack Size	Price	Availability
1 mg	$54	In Stock
5 mg	$85	In Stock
10 mg	$129	In Stock
25 mg	$229	In Stock
50 mg	$382	In Stock
100 mg	$562	In Stock
1 mL x 10 mM (in DMSO)	$61	In Stock

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Product Introduction

Bioactivity

Description	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).
Targets&IC50	MMP9:3 nM, MMP7:13 nM, MMP2:6 nM, MMP1:5 nM, MMP14:9 nM
In vitro	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]
In vivo	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]
Kinase Assay	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.
Alias	BB2516, KB-R8898, TA2516

Chemical Properties

Molecular Weight	331.41
Formula	C₁₅H₂₉N₃O₅
Cas No.	154039-60-8

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 33.1 mg/mL (100 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0174 mL	15.0871 mL	30.1741 mL	150.8705 mL
5 mM	0.6035 mL	3.0174 mL	6.0348 mL	30.1741 mL
10 mM	0.3017 mL	1.5087 mL	3.0174 mL	15.0871 mL
20 mM	0.1509 mL	0.7544 mL	1.5087 mL	7.5435 mL
50 mM	0.0603 mL	0.3017 mL	0.6035 mL	3.0174 mL
100 mM	0.0302 mL	0.1509 mL	0.3017 mL	1.5087 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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