PF-05089771 is a Nav1.7 channel blocker with IC50s of 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively. PF-05089771 exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. PF-05089771 blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro.
| Molecular Weight | 500.35 |
| Formula | C18H12Cl2FN5O3S2 |
| CAS Number | 1235403-62-9 |
| Solubility (25°C) | DMSO: ≥ 25 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 Sodium Channel Products |
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| ASN008
ASN008 is a permanently positively charged sodium channel blocker. |
| Psalmotoxin 1
Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). |
| Jingzhaotoxin-III
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. |
| Huwentoxin-IV
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. |
| Phrixotoxin 3
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. |
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