yingweiwo

Malotilate

Alias: NKK 105; CL-1500; Malotilate
Cat No.:V24961 Purity: ≥98%
Malotilate (NKK 105) is an orally bioactive hepatotropic agent and an antifibrotic substance that selectively inhibits 5-lipoxygenase (5-LOX) (IC50=4.7 μM).
Malotilate
Malotilate Chemical Structure CAS No.: 59937-28-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Product Description
Malotilate (NKK 105) is an orally bioactive hepatotropic agent and an antifibrotic substance that selectively inhibits 5-lipoxygenase (5-LOX) (IC50=4.7 μM). Malotilate prevents the development of hepatocellular damage in alcohol-pyrazole hepatitis by reducing hepatic acetaldehyde levels and preventing transferrin from being retained in hepatocytes.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Malotiate has the ability to decrease fibroblasts' in vitro cell migratory activity and collagen production [3]. Malotiate is an antifibrotic agent that concurrently promotes the 12- and 15-lipoxygenase pathways while selectively inhibiting 5-lipoxygenase. It has been demonstrated that malotiate protects against acute experimental liver damage brought on by a number of hepatotoxic substances, such as thioacetamide, carbon tetrachloride, ethanol, bromobenzene, and chloroform.
ln Vivo
Serum cholesterol levels quickly returned to normal after malotiate (100 mg/kg) was given orally to hypocholesterolemic rats once a day for three days [5].
Animal Protocol
Animal/Disease Models: SLC-SD strain male rats (rats with liver damage caused by carbon tetrachloride) [5]
Doses: 100 mg/kg
Route of Administration: Po; one time/day for 3 days
Experimental Results: Rats given CCI4 Hepatic triglyceride secretion was inhibited to approximately 40% of the levels in control rats. This suppression of triglyceride secretion completely normalized after 3 days of administration of malotiate.
References

[1]. Effects of malotilate on alcoholic liver injury in rats. Alcohol Clin Exp Res. 1988;12(5):665-670.

[2]. Vermeer MA, Wilson JH, Zijlstra FJ, Vincent JE. Differential effects of malotilate on 5-, 12- and 15-lipoxygenase in human ascites cells. Agents Actions. 1989;26(1-2):252-253.

[3]. Malotilate reduces collagen synthesis and cell migration activity of fibroblasts in vitro. Biochem Pharmacol. 1987;36(22):3957-3963.

[4]. Differential effects of malotilate on 5-, 12- and 15-lipoxygenase in human ascites cells. Eur J Pharmacol. 1989;159(3):291-295.

[5]. Action of malotilate on reduced serum cholesterol level in rats with carbon tetrachloride-induced liver damage. Jpn J Pharmacol. 1985;38(4):391-401.

Additional Infomation
Malotilate is an isopropyl ester.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H16O4S2
Molecular Weight
288.376
Exact Mass
288.049
CAS #
59937-28-9
PubChem CID
4006
Appearance
Light yellow to yellow solid powder
Density
1.3±0.1 g/cm3
Boiling Point
321.5±42.0 °C at 760 mmHg
Flash Point
138.7±15.9 °C
Vapour Pressure
0.0±0.7 mmHg at 25°C
Index of Refraction
1.562
LogP
3.83
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
6
Heavy Atom Count
18
Complexity
363
Defined Atom Stereocenter Count
0
InChi Key
YPIQVCUJEKAZCP-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H16O4S2/c1-7(2)15-10(13)9(11(14)16-8(3)4)12-17-5-6-18-12/h5-8H,1-4H3
Chemical Name
dipropan-2-yl 2-(1,3-dithiol-2-ylidene)propanedioate
Synonyms
NKK 105; CL-1500; Malotilate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 100 mg/mL (~346.76 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.4676 mL 17.3382 mL 34.6765 mL
5 mM 0.6935 mL 3.4676 mL 6.9353 mL
10 mM 0.3468 mL 1.7338 mL 3.4676 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Contact Us