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LR-90

Cat No.:V31245 Purity: ≥98%
LR-90 is an advanced glycation end product (AGE) inhibitor that can inhibit the inflammatory response of human monocytes.
LR-90
LR-90 Chemical Structure CAS No.: 245075-84-7
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
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Product Description
LR-90 is an advanced glycation end product (AGE) inhibitor that can inhibit the inflammatory response of human monocytes. LR-90 can also be used in studies of diabetic animal models.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
LR-90 dose-dependently reduced the expression of the genes for RAGE, MCP-1, COX-2, IP-10, and NOX2 after 1 hour of pretreatment. Four hours prior to S100b stimulation [1]. After 24 hours of pretreatment, 1 hour before to S100b stimulation, LR-90 (0, 25, 50, 100, and 200 μM) substantially and dose-dependently inhibited the adherence of THP-1 cells to endothelial cells [1]. THP-1 cell viability was unaffected by LR-90 (0, 25, 50, 100, and 200 μM) for a 24-hour period [1].
ln Vivo
LR-90 (50 mg/L, orally administered for 27 weeks) considerably decreases plasma lipids and has a certain influence on hyperglycemia in ZDF rats [2]. LR-90 (50 mg/L) decreases renal AGE, AGER and lipid peroxidation [2].
Cell Assay
Cell viability assay [1]
Cell Types: THP-1 Cell
Tested Concentrations: 0, 25, 50, 100 and 200 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: No cytotoxicity to THP-1 cells.

RT-PCR[1]
Cell Types: THP-1 Cell
Tested Concentrations: 0, 25, 50, 100 and 200 μM
Incubation Duration: 1 hour before adding S100b, for 4 hrs (hours)
Experimental Results: Dose-dependent inhibition of RAGE, MCP-mRNA expression1 , COX-2, IP-10 and NOX2 were stimulated with S100b.
Animal Protocol
Animal/Disease Models: Male ZDF rats (13 to 40 weeks) [2]
Doses: 50 mg/L
Route of Administration: Oral administration for 27 weeks.
Experimental Results: Plasma triacylglycerol and cholesterol were Dramatically diminished by approximately 55% and approximately 30% respectively. Mild effects on hyperglycemia and blood pressure. Lowered body weight.
References

[1]. Anti-inflammatory effects of the advanced glycation end product inhibitor LR-90 in human monocytes. Diabetes. 2007 Mar;56(3):647-55.

[2]. LR-90 prevents dyslipidaemia and diabetic nephropathy in the Zucker diabetic fatty rat. Diabetologia. 2008 May;51(5):882-91.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C35H34CL2N4O8
Molecular Weight
709.5725
Exact Mass
708.175
CAS #
245075-84-7
PubChem CID
10212249
Appearance
Typically exists as solid at room temperature
LogP
8.529
Hydrogen Bond Donor Count
6
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
12
Heavy Atom Count
49
Complexity
1060
Defined Atom Stereocenter Count
0
SMILES
ClC1=C(C([H])=C([H])C(=C1[H])C([H])([H])C1C([H])=C([H])C(=C(C=1[H])Cl)N([H])C(N([H])C1C([H])=C([H])C(=C([H])C=1[H])OC(C(=O)O[H])(C([H])([H])[H])C([H])([H])[H])=O)N([H])C(N([H])C1C([H])=C([H])C(=C([H])C=1[H])OC(C(=O)O[H])(C([H])([H])[H])C([H])([H])[H])=O
InChi Key
WJDMCXSGUCNRPZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C35H34Cl2N4O8/c1-34(2,30(42)43)48-24-11-7-22(8-12-24)38-32(46)40-28-15-5-20(18-26(28)36)17-21-6-16-29(27(37)19-21)41-33(47)39-23-9-13-25(14-10-23)49-35(3,4)31(44)45/h5-16,18-19H,17H2,1-4H3,(H,42,43)(H,44,45)(H2,38,40,46)(H2,39,41,47)
Chemical Name
2-[4-[[4-[[4-[[4-(2-carboxypropan-2-yloxy)phenyl]carbamoylamino]-3-chlorophenyl]methyl]-2-chlorophenyl]carbamoylamino]phenoxy]-2-methylpropanoic acid
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 (~140.93 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.52 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 (3.52 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 1.4093 mL 7.0465 mL 14.0930 mL
5 mM 0.2819 mL 1.4093 mL 2.8186 mL
10 mM 0.1409 mL 0.7047 mL 1.4093 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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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