1642112-31-9
1642112-31-9 structure
- Name: AMG8379
- Chemical Name: 1-(3'-Chloro-2,5'-difluoro-5-methoxy-4-biphenylyl)-N-(1,2-oxazol-3-yl)-2-oxo-1,2-dihydro-6-quinolinesulfonamide
- CAS Number: 1642112-31-9
- Molecular Formula: C25H16ClF2N3O5S
- Molecular Weight: 543.926
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
- Create Date: 2020-01-12 10:45:49
- Modify Date: 2024-01-14 16:22:53
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AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM; potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays; displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5; blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking; exhibits pharmacodynamic effects in translatable models of both itch and pain.
| Name | 1-(3'-Chloro-2,5'-difluoro-5-methoxy-4-biphenylyl)-N-(1,2-oxazol-3-yl)-2-oxo-1,2-dihydro-6-quinolinesulfonamide |
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| Synonyms |
6-Quinolinesulfonamide, 1-(3'-chloro-2,5'-difluoro-5-methoxy[1,1'-biphenyl]-4-yl)-1,2-dihydro-N-3-isoxazolyl-2-oxo-
1-(3'-Chloro-2,5'-difluoro-5-methoxy-4-biphenylyl)-N-(1,2-oxazol-3-yl)-2-oxo-1,2-dihydro-6-quinolinesulfonamide |
| Description | AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM; potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays; displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5; blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking; exhibits pharmacodynamic effects in translatable models of both itch and pain. |
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| Related Catalog | |
| In Vitro | AMG8379 is 100 to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in heart, as well as TTX-resistant NaV channels in DRG neurons[1]. The IC50 for AMG8379 inhibition of C-fiber spiking based on the level of firing in NaV1.7 KO mice representing complete pharmacological block of the NaV1.7-component of this assay is calculated. In this manner, the IC50 for AMG8379 block is 47.0 ± 8.1 nM[1]. |
| In Vivo | AMG8379 (30-100 mg/kg; p.o.) inhibits Capsaicin-induced nociceptive behavior[1]. Animal Model: CD-1 male mice[1] Dosage: 30 or 100 mg/kg body weight Administration: Oral Result: Showed a dose-dependent reduction in overall nociceptive behavior. |
| References |
| Density | 1.5±0.1 g/cm3 |
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| Boiling Point | 752.0±70.0 °C at 760 mmHg |
| Molecular Formula | C25H16ClF2N3O5S |
| Molecular Weight | 543.926 |
| Flash Point | 408.6±35.7 °C |
| Exact Mass | 543.046753 |
| LogP | 4.78 |
| Vapour Pressure | 0.0±2.5 mmHg at 25°C |
| Index of Refraction | 1.656 |