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Ki16425

Cat. No. M2213
Ki16425 Structure
Size Price Availability Quantity
10mg USD 110  USD110 In stock
50mg USD 440  USD440 In stock
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Quality Control & Documentation
Biological Activity

Ki16425 is an antagonist of the lysophosphatidic acid receptors LPA1 and LPA3. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts and A431 cells. Ki16425 also inhibited LPA-induced long-term responses, including DNA synthesis and cell migration. Ki16425 reduced the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Significantly, Ki16425 also reduced the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth.

Chemical Information
Molecular Weight 474.96
Formula C23H23ClN2O5S
CAS Number 355025-24-0
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Moughal NA, et al. J Neurochem. Protean agonism of the lysophosphatidic acid receptor-1 with Ki16425 reduces nerve growth factor-induced neurite outgrowth in pheochromocytoma 12 cells.

[2] Ohta H, et al. Mol Pharmacol. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.

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