| Identification | Back Directory | [Name]
Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]- | [CAS]
2241651-99-8 | [Synonyms]
AZ194
CRMP2-Ubc9-NaV1.7 inhibitor 194
Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]- | [Molecular Formula]
C34H31F2N3O3 | [MOL File]
2241651-99-8.mol | [Molecular Weight]
567.64 |
| Chemical Properties | Back Directory | [Boiling point ]
759.2±60.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 33.33 mg/mL (58.72 mM; Need ultrasonic) | [form ]
Solid | [pka]
5.11±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects[1]. | [in vivo]
AZ194 would provide pain relief in rat models of chemotherapy- and nerve injury- induced neuropathic pain. AZ194 (orally; at 2 and 10 mg/kg) restores mechanical sensitivity in animals with chemotherapy-induced and nerve injury-induced neuropathic nociception[1].
AZ194 (10 mg/kg; ip; CD1 male mice) does not affect motor performance (open field). AZ194 synergizes with commonly used painkillers, engages NaV1.7-dependent endogenous opioid signaling[1]. | [IC 50]
Nav1.7 | [storage]
Store at -20°C | [References]
[1] Cai S, et al. Selective targeting of NaV1.7 via inhibition of the CRMP2-Ubc9 interaction reduces pain in rodents. Sci Transl Med. 2021;13(619):eabh1314. DOI:10.1126/scitranslmed.abh1314 |
|
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|