Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]-

Product Name: Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]-
CAS No.: 2241651-99-8
Chemical Name: Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]-
Synonyms: AZ194;HUN51998;AZ194, 10 mM in DMSO;CRMP2-Ubc9-NaV1.7 inhibitor 194;2-(1-{4-[(3-fluorophenyl)methoxy]-3-methoxybenzoyl}piperidin-4-yl)-1-[(3-fluorophenyl)methyl]-1H-1,3-benzodiazole;(4-(1-(3-Fluorobenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)(4-((3-fluorobenzyl)oxy)-3-methoxyphenyl)methanone;Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]-;nociceptive neurotransmission,Inhibitor,CRMP2-Ubc9 interaction,Na+ channels,Na channels,inhibit,AZ-194,Sodium Channel,pain,AZ 194,antinociceptive effects,sensory neurons,AZ194
CBNumber: CB310017615
Molecular Formula: C34H31F2N3O3
Formula Weight: 567.64
MOL File: 2241651-99-8.mol

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Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]- Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]- Chemical Properties,Usage,Production

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

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

Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]- Preparation Products And Raw materials

Raw materials

Preparation Products

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Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]- Suppliers

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2241651-99-8, Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]-Related Search:

Methanone, [4-[(3-fluorophenyl)methoxy]-3-methoxyphenyl][4-[1-[(3-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-1-piperidinyl]-

CRMP2-Ubc9-NaV1.7 inhibitor 194

AZ194

nociceptive neurotransmission,Inhibitor,CRMP2-Ubc9 interaction,Na+ channels,Na channels,inhibit,AZ-194,Sodium Channel,pain,AZ 194,antinociceptive effects,sensory neurons,AZ194

(4-(1-(3-Fluorobenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)(4-((3-fluorobenzyl)oxy)-3-methoxyphenyl)methanone

2-(1-{4-[(3-fluorophenyl)methoxy]-3-methoxybenzoyl}piperidin-4-yl)-1-[(3-fluorophenyl)methyl]-1H-1,3-benzodiazole

AZ194, 10 mM in DMSO

HUN51998

2241651-99-8

C34H31F2N3O3