yingweiwo

LUF6096

Alias: LUF6096 LUF 6096LUF-6096CF-602 CF602 CF 602
Cat No.:V12661 Purity: ≥98%
LUF6096 is a potent allosteric enhancer of adenosine A3 receptor.
LUF6096
LUF6096 Chemical Structure CAS No.: 1116652-18-6
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
Other Sizes
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
Purity & Quality Control Documentation

Purity: ≥98%

Product Description
LUF6096 is a potent allosteric enhancer of adenosine A3 receptor. LUF6096 displays low orthosteric affinity for any adenosine receptor. LUF6096 has protective effects in myocardial ischemia/reperfusion injury.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
The dissociation rate of 125I-AB-MECA from A3 receptors in CHO cell membranes is halved by 2.5 times with LUF6096 (10 μM; 30-120 minutes) [1]. Forskolin-stimulated cAMP generation in CHO cells can be inhibited and the intrinsic activity of Cl-IB-MECA considerably enhanced by LUF6096 (10 μM; 15 min pretreatment) [1].
ln Vivo
In dogs, myocardial ischemia/reperfusion damage is prevented by LUF6096 (two intravenous bolus doses of 0.5 mg/kg or a single intravenous bolus dosage of 1 mg/kg) [1].
Animal Protocol
Animal/Disease Models: Adult mongrel dogs (15-25 kg) underwent left anterior descending (LAD) coronary artery occlusion and reperfusion [1]
Doses: Two intravenous (iv) (iv)bolus injections of 0.5 mg/kg or a single intravenous (iv) (iv)bolus of 1 mg/kg given Medication: intravenous (iv) (iv)bolus
Experimental Results: Infarct size was Dramatically diminished (approximately 50% reduction) compared to vehicle-treated dogs.
References
[1]. Heitman LH, et, al. A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor. J Med Chem. 2009 Feb 26;52(4):926-31.
[2]. Du L, et, al. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor. J Pharmacol Exp Ther. 2012 Jan;340(1):210-7.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H21CL2N3O
Molecular Weight
414.33
Exact Mass
413.106
CAS #
1116652-18-6
Related CAS #
1116652-18-6;
PubChem CID
25191023
Appearance
Typically exists as solid at room temperature
LogP
6.875
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
4
Heavy Atom Count
28
Complexity
528
Defined Atom Stereocenter Count
0
SMILES
ClC=1C=CC(=CC1Cl)N=C2NC3=CC=CC=C3C(=C2)NC(C4CCCCC4)=O
InChi Key
UWEIQVQNNLVOEI-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H21Cl2N3O/c23-17-11-10-15(12-18(17)24)25-21-13-20(16-8-4-5-9-19(16)26-21)27-22(28)14-6-2-1-3-7-14/h4-5,8-14H,1-3,6-7H2,(H2,25,26,27,28)
Chemical Name
N-[2-[(3,4-Dichlorophenyl)amino]-4-quinolinyl]-cyclohexanecarboxamide
Synonyms
LUF6096 LUF 6096LUF-6096CF-602 CF602 CF 602
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 : ~20 mg/mL (~48.27 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2 mg/mL (4.83 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 20.0 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 2.4135 mL 12.0677 mL 24.1354 mL
5 mM 0.4827 mL 2.4135 mL 4.8271 mL
10 mM 0.2414 mL 1.2068 mL 2.4135 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.

Biological Data
  • Measurement of LUF6096 plasma levels by LC-MS. A, chromatogram showing the retention times of LUF6096 and the internal standard LUF6093 after separation by high-performance liquid chromatography and detection by MS. B, mass spectra of LUF6093 and LUF6096. The arrows point to strong (M + H) signals at 414.01 for LUF6096 and 385.99 for LUF6093. C, calibration curve used to calculate the plasma levels of LUF6096.[2]. Du L, et, al. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor. J Pharmacol Exp Ther. 2012 Jan;340(1):210-7.
  • Effect of LUF6096 on [35S]GTPγS binding in assays with the canine A3 AR. Incubations were started by the addition of the membrane suspension (5 μg of protein) as described under Materials and Methods and carried out in quadruplicate for 2 h at 25°C. The membrane solutions were preincubated with LUF6096 for 30 min at 25°C before the addition of ∼0.1 nM [35S]GTPγS. A, the effect of increasing concentrations of LUF6096 on [35S]GTPγS binding in response to a maximal concentration of Cl-IB-MECA (10−5 M) (n = 9). B, stimulation of [35S]GTPγS binding by increasing concentrations of Cl-IB-MECA in the absence (control) or presence of LUF6096 (10 μΜ) (n = 6). C, stimulation of [35S]GTPγS binding in response to increasing concentrations of adenosine in the absence (control) or presence of LUF6096 (10 μΜ) (n = 5).[2]. Du L, et, al. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor. J Pharmacol Exp Ther. 2012 Jan;340(1):210-7.
  • Effect of LUF6096 on equilibrium orthosteric radioligand binding to the canine A1 (A), A2A (B), and A3 (C) ARs. Membranes (50 μg) were incubated with [125I]I-AB-MECA (∼0.5 nM; A1 and A3 ARs) or [3H]CGS21680 (∼10 nM; A2A ARs) for 2 h at room temperature in the presence of increasing concentrations of LUF6096. Nonspecific binding was determined with 200 μM adenosine-5′-N-ethylcarboxamide. The data shown are representative of three independent experiments.[2]. Du L, et, al. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor. J Pharmacol Exp Ther. 2012 Jan;340(1):210-7.
Contact Us