SML2698

EVT-101 dihyrochloride

≥98% (HPLC)

• Synonym(e): 5-(3-Difluoromethyl-4-fluorophenyl)-3-(2-methylimidazol-1-ylmethyl)pyridazine dihydrochloride, 5-[3-(Difluoromethyl)-4-fluorophenyl]-3-[(2-methyl-1H-imidazol-1-yl)methyl]pyridazine dihydrochloride, EVT 101 dihydrochloride, EVT101 dihydrochloride
• Empirische Formel (Hill-System): C₁₆H₁₃F₃N₄ · 2HCl
• CAS-Nummer: 1189088-41-2
• Molekulargewicht: 391.22
• NACRES: NA.77
• UNSPSC Code: 12352200
• eCl@ss: 32160702
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Eigenschaften

• assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: H₂O: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: FC(F)C1=C(F)C=CC(C2=CC(CN3C(C)=NC=C3)=NN=C2)=C1
• InChI: 1S/C16H13F3N4.2ClH/c1-10-20-4-5-23(10)9-13-6-12(8-21-22-13)11-2-3-15(17)14(7-11)16(18)19;;/h2-8,16H,9H2,1H3;2*1H
• InChI key: OJBLXSPBJMGZDN-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

EVT-101 is a potent and orally active NR2B-subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist (IC₅₀ = 17 nM against 5 nM Ro 25-6981 for binding rat brain membrane) that targets the GluN1/GluN2B dimer interface with a distinctly different binding mode as ifenprodil. EVT 101 potently inhibits current induction by Glu/Gly (100 μM each) in rat GluN1-1a/mouse GluN2B co-expressing xenopus in vitro (IC₅₀ = 12 nM) and blocks MK-801 binding in mouse brain in vivo (3 mg EVT-101/kg p.o. & 0.2 μCi [3H]MK-801/g i.v. administered 55 min and 10 min prior to brain removal, respectively).

Potent and orally active NR2B-/GluN2B-subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist with in vitro and in vivo efficacy.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable