Brequinar Sodium (Bipenquinate, BRQ, DUP-785, NSC 368390) is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of ~20 nM and triggers differentiation in the ER-HoxA9, U937, and THP1 cells with ED50 of ~1 μM.
| Molecular Weight | 397.35 |
| Formula | C23H14F2NNaO2 |
| CAS Number | 96201-88-6 |
| Solubility (25°C) | DMSO 79 mg/mL Water 26 mg/mL |
| 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 DHODH Products |
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| DHODH-IN-13
DHODH-IN-13 is a hydroxyfurazan analog of A771726 and a dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 4.3 μM for hepatic DHODH in rats.DHODH-IN-13 can be used in rheumatoid arthritis-related studies. |
| DHODH-IN-12
DHODH-IN-12 is a Leflunomide derivative and a weak inhibitor of dihydroorotic acid dehydrogenase (DHODH), with a pKa of 5.07. |
| hDHODH-IN-5
hDHODH-IN-5 is a human dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 0.91 μM. hDHODH-IN-7 induces differentiation of acute myeloid leukemia cells. |
| DHODH-IN-8
DHODH-IN-8 is an inhibitor of human and Plasmodium falciparum dihydroorotic acid dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM and Ki of 0.016 μM and 5.6 μM, respectively.DHODH-IN-8 exhibits antimalarial activity. |
| DHODH-IN-14
DHODH-IN-14 is a hydroxyfurazan analog of A771726 and a dihydroorotic acid dehydrogenase (DHODH) inhibitor with an IC50 of 0.49 μM for hepatic DHODH in rats.DHODH-IN-14 can be used in rheumatoid arthritis-related studies. |
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