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SC 57461

Alias: SC57461; SC-57461; SC 57461
Cat No.:V14449 Purity: ≥98%
SC-57461A is an orally bioactive, non-peptide, selective leukotriene A4 (LTA4) hydrolase inhibitor (antagonist) with IC50s of 2.5 nM, 3 nM and 3 nM for recombinant human, mouse and mouse LTA4 hydrolase, respectively.
SC 57461
SC 57461 Chemical Structure CAS No.: 423169-68-0
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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Product Description
SC-57461A is an orally bioactive, non-peptide, selective leukotriene A4 (LTA4) hydrolase inhibitor (antagonist) with IC50s of 2.5 nM, 3 nM and 3 nM for recombinant human, mouse and mouse LTA4 hydrolase, respectively. 23 nM.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In whole blood, SC-57461A suppresses the synthesis of LTB4 induced by ionophores with IC50 values of 49, 166, and 466 nM for human, mouse, and topovirus, respectively [1]. The LTA4 fine-tuned enzyme (IC50=2.5 nM) and entire cells (IC50=49 nM) are both effectively inhibited by SC-57461A [2].
ln Vivo
SC-57461A also showed excellent effects in in vitro mouse experiments, inhibiting the production of LTB4 with ED50=0.2 mg/kg and ED90=1 mg/kg. SC-57461A also inhibits LTB4 production in the peritoneal model with ED50=1 mg/kg[2]. SC-57461A is a potent, selective, competitive inhibitor of the LTA4 disinfecting enzyme with excellent activity in whole animals. SC-57461A in mice and mice
Animal Protocol
Animal/Disease Models: Fasted CD rat [3]
Doses: 0.01, 0.1, 1 and 10 mg/kg
Route of Administration: Oral
Experimental Results: ED50 value at 1.0 is 0.2 mg/kg . h and 0.8 mg/kg at 3.0 h. A single dose of 10 mg/kg prevented 79%, 67% and 44% of LTB4 production at 6 hrs (hrs (hours)), 18 hrs (hrs (hours)) and 24 hrs (hrs (hours)), respectively.
References

[1]. Pharmacological characterization of SC-57461A (3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid HCl), a potent and selective inhibitor of leukotriene A(4) hydrolase I: in vitro studies. J Pharmacol Exp Ther. 2002 Feb;300(2):577-82.

[2]. T D Penning. Inhibitors of leukotriene A4 (LTA4) hydrolase as potential anti-inflammatory agents. Curr Pharm Des. 2001 Feb;7(3):163-79.

[3]. Pharmacological characterization of SC-57461A (3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid HCl), a potent and selective inhibitor of leukotriene A(4) hydrolase II: in vivo studies. J Pharmacol Exp Ther. 2002 Feb;300(2):583-7.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H25NO3
Molecular Weight
327.42
Exact Mass
363.16
CAS #
423169-68-0
PubChem CID
9820433
Appearance
White to off-white solid powder
Density
1.115g/cm3
Boiling Point
499.7ºC at 760 mmHg
Flash Point
256.01ºC
Index of Refraction
1.562
LogP
4.254
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
10
Heavy Atom Count
25
Complexity
347
Defined Atom Stereocenter Count
0
Synonyms
SC57461; SC-57461; SC 57461
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

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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 : ~250 mg/mL (~687.04 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.72 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 20.8 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: ≥ 2.08 mg/mL (5.72 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 20.8 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.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (5.72 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 20.8 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 3.0542 mL 15.2709 mL 30.5418 mL
5 mM 0.6108 mL 3.0542 mL 6.1084 mL
10 mM 0.3054 mL 1.5271 mL 3.0542 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:

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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?
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  • Enter 5 in the Volume box and choose the correct unit (mL)
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  • 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)
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  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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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.)
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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.

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