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About This Item
실험식(Hill 표기법):
C24H22F2N2O2
CAS Number:
Molecular Weight:
408.44
UNSPSC 코드:
12352200
NACRES:
NA.77
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
2-8°C
SMILES string
NC(C1=CC=C(OC2=CC=C(CN3CCC[C@H]3C4=CC=CC(F)=C4)C=C2)C(F)=C1)=O
InChI
1S/C24H22F2N2O2/c25-19-4-1-3-17(13-19)22-5-2-12-28(22)15-16-6-9-20(10-7-16)30-23-11-8-18(24(27)29)14-21(23)26/h1,3-4,6-11,13-14,22H,2,5,12,15H2,(H2,27,29)/t22-/m0/s1
InChI key
WHHMECUDUQRPJT-QFIPXVFZSA-N
생화학적/생리학적 작용
Brain-penetrant, orally active, short-acting, high-affinity, potent and selective κ (kappa) opioid receptor (KOR) antagonist with in vitro and in vivo efficacy.
LY2444296 is a brain-penetrant, orally active, short-acting, high-affinity, potent and selective κ (kappa) opioid receptor (KOR) antagonist (human κ/μ/δ Ki = 0.565/35.8/211 nM against diprenorphine binding; GTP-γ-S binding IC50/agonist/subtype transfectant = 1.57 nM/300 nM U69593/κ, 21.3 nM/1 μM DAMGO/μ 293 nM/30 nM DPDPE/d). LY2444296 reverses κ agonist antinociceptive efficacy in vivo (ED50 = 0.24 mg/kg p.o. against 1 mg/kg U69593 sc. by rat formalin test), decreases immobility time (10 or 30 mg/kg sc.) and prevents enhanced alcohol consumption (5 mg/kg i.p.) among mice subjected to stress by forced swimming.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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