Ki16198; Ki-16198; Ki 16198
| 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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| 500mg |
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| Other Sizes |
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Purity: ≥98%
Ki16198 (Ki 16198; Ki-16198), the methyl ester of Ki16425, is a potent LPA (Lysophosphatidic acid) receptor antagonist with important biological activity. It suppresses the production of inositol phosphate induced by LPA1 and LPA3, with Ki values of 0.34 μM and 0.93 μM, respectively.
| Targets |
LPA1 receptor ( Ki = 0.34 μM ); LPA1 receptor ( Ki = 0.34 μM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
On collagen-coated 12-well dishes, RH7777 cells expressing LPA1, LPA2, LPA3, LPA4, or LPA5 are cultured in the growth medium. After that, the medium is changed to TCM199 containing 2 μCi/mL [3H]inositol and 0.1% (w/v) BSA (fraction V). The cells are then incubated for 30 minutes with the indicated concentrations of Ki16425 or Ki16198 with or without 1 μM LPA in the presence of 10 mM LiCl in the same medium at a final volume of 0.5 mL. Twenty-four hours later, the cells are rinsed three times with HEPES-buffered medium, which consisted of 20 mM Hepes (pH 7.4), 134 mM NaCl, 4.7 mM KCl, 1.2 mM KH2PO4, 1.2 mM MgSO4, 2.5 mM NaHCO3, 5 mM glucose, and 0.1% (w/v) BSA. The cells are frozen and 1 N HCl (0.1 mL) is added to stop the reaction. The [3H]inositol phosphate fractions are separated using the supernatant (0.5 mL of acid extract) of the thawed cells. The data are normalized to 105 dpm of the total radioactivity that is integrated into the inositol lipids in cells. The total radioactivity of the trichloroacetic acid (5%)-insoluble fraction is determined.
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| Cell Assay |
On 12-well plates, YAPC-PD or Panc-1 cells are seeded at a density of 1 × 104 cells per milliliter. A change to RPMI1640 containing 0.1% BSA is made to the medium sixteen hours prior to the experiments. The cells are then stimulated in the same medium, with or without Ki16198, for a duration of 24 hours. The ability of the cells to reduce MTT (3-(4,5-Dimethyl-2-thiazoyl)-2,5-diphenyltetrazolium bromide) is used to measure the proliferation activity.
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| Animal Protocol |
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| References |
| Molecular Formula |
C24H25CLN2O5S
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| Molecular Weight |
488.98
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| Exact Mass |
488.12
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| Elemental Analysis |
C, 58.95; H, 5.15; Cl, 7.25; N, 5.73; O, 16.36; S, 6.56
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| CAS # |
355025-13-7
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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)OC
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| InChi Key |
HHVJBROTJWPHHX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H25ClN2O5S/c1-15-22(26-24(29)31-16(2)19-6-4-5-7-20(19)25)23(32-27-15)18-10-8-17(9-11-18)14-33-13-12-21(28)30-3/h4-11,16H,12-14H2,1-3H3,(H,26,29)
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| Chemical Name |
methyl 3-[[4-[4-[1-(2-chlorophenyl)ethoxycarbonylamino]-3-methyl-1,2-oxazol-5-yl]phenyl]methylsulfanyl]propanoate
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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 (5.11 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (5.11 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (5.11 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: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0451 mL | 10.2254 mL | 20.4507 mL | |
| 5 mM | 0.4090 mL | 2.0451 mL | 4.0901 mL | |
| 10 mM | 0.2045 mL | 1.0225 mL | 2.0451 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.
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