Molecular Formula | C23H23ClN2O5S |
Molar Mass | 474.96 |
Density | 1.353 |
Melting Point | 59.5-60.5°C |
Boling Point | 623.7±55.0 °C(Predicted) |
Solubility | DMSO: 16mg/mL |
Appearance | solid |
Color | white |
pKa | 4.32±0.10(Predicted) |
Storage Condition | -20°C |
In vitro study | Kil6425 preferentially inhibits LPA1 and LPA3 regulated responses, but has only moderate effect on lpa2. Ki16425 inhibited LPA-induced Ca2 responses in THP-1 cells, 3T3 fibroblasts, and A431 cells, but had only minor effects on PC-12 and HL-60 cells, this indicates that Ki16425 can be used to evaluate specific LPA receptors that have a short-term effect on LPA. Ki16425 acts on Swiss 3T3 fibroblasts to inhibit long-term DNA synthesis and LPA-induced cell migration. Ki1642 reduces LPA-induced activation of p42/p44 MAPK, which can be used as a weak activator of p42/p44 MAPK. The effect of Ki16425 on PC-12 cells also significantly decreased the activation of p42/p44 MAPK induced by NGF, and inhibited NGF-induced neural proliferation. Ki16425 significantly inhibited the expression of COX-2 protein induced by synovial fluid. Ki16425 also inhibited COX-2 expression by IL-1 of the enhancement of LPA. Kil6425 preferentially inhibits LPA1 and LPA3-regulated responses, but only has a moderate effect on lpa2. Ki16425 acts on THP-1 cells, 3T3 fibroblasts, and A431 cells, inhibiting LPA-induced Ca Ki1642 reduces LPA-induced activation of p42/p44 MAPK, and can act as a weak activator of p42/p44 MAPK. The effect of Ki16425 on PC-12 cells also significantly decreased the activation of p42/p44 MAPK induced by NGF, and inhibited NGF-induced neural proliferation. Ki16425 significantly inhibited the expression of COX-2 protein induced by synovial fluid. Ki16425 also inhibited COX-2 expression by IL-1 of the enhancement of LPA. |
In vivo study | Ki16425 (30 mg/kg, I. P.) completely inhibited LPA-induced neuropathic behavior, pre-treatment with lysophosphatidic acid for 30 minutes, but not 90 minutes, indicating that Ki16425 is a transient inhibitor. Ki16425 acts on the dorsal root ganglion and also inhibits the upregulation of caα2t-1 induced by nerve injury, and acts on the spinal dorsal horn to inhibit the decrease of SP immune response. Ki16425 (30 mg/kg, I. P.) completely inhibited LPA-induced neuropathic behavior, pre-treated with lysophosphatidic acid for 30 minutes, but not 90 minutes, indicating that Ki16425 is a transient inhibitor. Ki16425 acts on the dorsal root ganglion and also inhibits the upregulation of caα2t-1 induced by nerve injury, and acts on the spinal dorsal horn to inhibit the decrease of SP immune response. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
HS Code | 29349990 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.105 ml | 10.527 ml | 21.054 ml |
5 mM | 0.421 ml | 2.105 ml | 4.211 ml |
10 mM | 0.211 ml | 1.053 ml | 2.105 ml |
5 mM | 0.042 ml | 0.211 ml | 0.421 ml |