XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).
| Molecular Weight | 516.37 |
| Formula | C23H15F7N2O4 |
| CAS Number | 1873358-87-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 ROR Products |
|---|
| JTE-151
JTE-151 is a RORγ inhibitor that suppresses overactive immune responses by inhibiting RORγ associated with Th17 cell activation.JTE-151 can be used in studies related to autoimmune diseases. |
| SAR-441169
SAR-441169 is a RORγt inverse agonist that can be used in studies related to psoriasis. |
| GRC-39815
GRC-39815 is a RORγt inverse agonist that can be used in studies related to chronic obstructive pulmonary disease. |
| RORγ antagonist 1
RORγ antagonist 1, a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). |
| RORγt inverse agonist 31
RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 0.428 μM. |
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