Ro 6842262 (LPA1 receptor antagonist 1) is an orally bioavailable, highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM. Ro 6842262 attenuates NHLF human lung fibroblast cell proliferation and contraction in vitro. Ro 6842262 also reduces plasma histamine levels in mouse LPA-challenge model.
| Molecular Weight | 482.53 |
| Formula | C28H26N4O4 |
| CAS Number | 1396006-71-5 |
| Storage | Store at -20°C |
| 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.
| Related LPL Receptor Products |
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| Ceranib-2
Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 decreases levels of sphingosine and S1P, induces cell apoptosis and exhibits anticancer activity. |
| BMS-986234
BMS-986234 is a lysophosphatidic acid receptor-1 (LPA1) antagonist with a Kb value of 2.8 ± 0.4 nM. |
| BMS-986337
BMS-986337 is a lysophosphatidic acid receptor (LPAR1) antagonist for studies related to pulmonary fibrosis. |
| DJS-002
DJS-002 is an LPA1 receptor antagonist that may be used in studies related to idiopathic pulmonary fibrosis (IPF). |
| HL001
HL001 is an LPA1 receptor antagonist that may be used in studies related to idiopathic pulmonary fibrosis (IPF). |
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