Shopping Cart

Your shopping cart is currently empty

Cilastatin

Name: Cilastatin
Brand: TargetMol
SKU: T2583
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

🥰Excellent

Catalog No. T2583Cas No. 82009-34-5

Alias MK0791

Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.

Cilastatin

Copy Product Info

🥰Excellent

Purity: 99.71%

Catalog No. T2583Alias MK0791Cas No. 82009-34-5

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$30	In Stock	In Stock
10 mg	$37	In Stock	In Stock
25 mg	$57	In Stock	In Stock
50 mg	$81	In Stock	In Stock
100 mg	$126	In Stock	In Stock
200 mg	$198	In Stock	In Stock
500 mg	$343	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

Questions

Batch Information

Select Batch

Purity:99.71%

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Cilastatin AI Summary

Cilastatin exhibits a protective bioactivity against lethal systemic infection by Staphylococcus aureus 8008 (MRSA) in ICR mice with an ED50 of 7.88 mg/kg when administered subcutaneously. It shows inhibitory activity against beta-lactamase renal dipeptidase with Ki values of 190.0 nM, 110.0 nM, and 210.0 nM. Pharmacokinetic data in humans reveal a total body clearance of 2.3 mL.min-1.kg-1 and renal clearance of 0.41 mL.min-1.kg-1, with a volume of distribution at steady state of 0.15 L/kg, a fraction unbound of 0.6, a half-life of 0.86 hours, and a mean residence time of 1.1 hours. Cilastatin inhibits Bacillus subtilis Sfp phosphopantetheinyl transferase with a potency of 79,432.8 nM and shows various degrees of inhibitory activity against TP_TRANSPORTER, PHA uptake, and ES uptake in different expressing S2 cells. It also exhibits potential antiviral properties by showing inhibition against SARS-CoV-2 3CL-Pro protease and cytotoxicity in VERO-6 cells, though with moderate efficacy. Additionally, the compound shows antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 0.16 ug/mL and inhibitory activities in human HDAC6 assays. Cilastatin displays variable effects on cell growth rates across different cell types and interacts with protein domains affecting their thermal stability. However, it does not show significant bioactivity across various human and rat receptors and enzymatic assays, as results were above 30,000.0 nM..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.
Targets&IC50	Metallob-lactamase enzyme CphA (bacterial):178 μM (IC50), Renal dehydropeptidase I:0.1 μM (IC50)
Synonyms	MK0791

Chemical Properties

Molecular Weight	358.45
Formula	C₁₆H₂₆N₂O₅S
Cas No.	82009-34-5
Smiles	CC1(C)C[C@@H]1C(=O)N\C(=C/CCCCSC[C@H](N)C(O)=O)C(O)=O
Relative Density.	1.275 g/cm3

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 250 mg/mL (697.45 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.58 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7898 mL	13.9489 mL	27.8979 mL	139.4895 mL
5 mM	0.5580 mL	2.7898 mL	5.5796 mL	27.8979 mL
10 mM	0.2790 mL	1.3949 mL	2.7898 mL	13.9489 mL
20 mM	0.1395 mL	0.6974 mL	1.3949 mL	6.9745 mL
50 mM	0.0558 mL	0.2790 mL	0.5580 mL	2.7898 mL
100 mM	0.0279 mL	0.1395 mL	0.2790 mL	1.3949 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc