Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Ki16425 (also called Ki 16425; Debio-0719; Ki-16425; Debio 0719) is a competitive, selective and reversible antagonist of LPA which inhibits LPA1, LPA2 and LPA3 with Ki values of 0.34 μM, 6.5 μM and 0.93 μM in RH7777 cell lines, respectively. Ki16425 inhibits neurite outgrowth induced by nerve growth factor in pheochromocytoma 12 cells. ki16425 reduces inflammation in the abdomen and throughout the body in a mouse model of peritoneal sepsis.
Targets |
LPA1 ( Ki = 0.34 μM ); LPA3 ( Ki = 0.93 μM ); LPA2 ( Ki = 6.5 μM )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
The inositol phosphates (sum of inositol bisphosphate and inositol trisphosphate) were measured after 1 minute of incubation of RH7777 cells with or without Ki16425. The radioactivity of the trichloroacetic acid(5%)-insoluble fraction was taken into consideration as the total radioactivity, and the results were normalized to 105 dpm of the total radioactivity incorporated into the cellular inositol lipids.
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Cell Assay |
Ki16425 suppressed the expression of heparin-binding EGF-like growth factor (HB-EGF) in human breast and prostate cancer cells.
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Animal Protocol |
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References |
Molecular Formula |
C23H23CLN2O5S
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Molecular Weight |
474.96
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Exact Mass |
474.1
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Elemental Analysis |
C, 58.16; H, 4.88; Cl, 7.46; N, 5.90; O, 16.84; S, 6.75
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CAS # |
355025-24-0
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)CSCCC(=O)O
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InChi Key |
LLIFMNUXGDHTRO-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H23ClN2O5S/c1-14-21(25-23(29)30-15(2)18-5-3-4-6-19(18)24)22(31-26-14)17-9-7-16(8-10-17)13-32-12-11-20(27)28/h3-10,15H,11-13H2,1-2H3,(H,25,29)(H,27,28)
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Chemical Name |
3-[[4-[4-[1-(2-chlorophenyl)ethoxycarbonylamino]-3-methyl-1,2-oxazol-5-yl]phenyl]methylsulfanyl]propanoic acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.26 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 (5.26 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 (5.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO +95%Corn oil : 30 mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1054 mL | 10.5272 mL | 21.0544 mL | |
5 mM | 0.4211 mL | 2.1054 mL | 4.2109 mL | |
10 mM | 0.2105 mL | 1.0527 mL | 2.1054 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.
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.
Inhibitory effect of antagonist (Ki16425) for LPA receptor on the LPA- and synovial fluid-induced COX-2 expression in RA synovial cells. J Immunol . 2008 Oct 1;181(7):5111-9. td> |