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经验公式(希尔记法):
C21H24N2O2 · HCl
化学文摘社编号:
分子量:
372.89
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI
1S/C21H24N2O2.ClH/c1-13-4-6-17-16(10-13)15-8-9-22-18(21(15)23-17)11-14-5-7-19(24-2)20(12-14)25-3;/h4-7,10,12,18,22-23H,8-9,11H2,1-3H3;1H
SMILES string
CC1=CC(C2=C(C(NCC2)CC(C=C3OC)=CC=C3OC)N4)=C4C=C1.Cl
InChI key
BKAZOTIBKRWLQA-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
High-affinity, 5-HT2B subtype-selective serotonin receptor antagonist with in vitro and in vivo efficacy.
LY272015 is a high-affinity, 5-HT2B subtype-selective serotonin receptor antagonist (5-HT2B -log KB = 9.86, 5-HT2A/5-HT2C -log Ki = 7.65/7.92) that exhibits antihypertensive efficacy in deoxycorticosterone acetate (DOCA)-salt-hypertensive rats in vivo (1, 3 mg/kg iv; 1x/wk for 4 wks). LY272015 inhibits mitral valve interstitial cell (MVIC) activation by 5HT in cultures (100 nM LY, 10 nM or 1 μM 5HT; canine MVIC) and ex vivo (100 μM LY, 10 μM 5HT; human MV), as well as mitigates angiotensin II infusion-provoked MV remodeling in mice in vivo (3 mg/kg via infusion by osmotic pumps 2x/wk).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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