SML2255
BI-2545
≥98% (HPLC)
别名:
(1R,5S,6S)-3,5-bis(Trifluoromethyl)benzyl 6-((1H-benzo[d][1,2,3]triazole-5-carboxamido)methyl)-3-azabicyclo[3.1.0]hexane-3-carboxylate, [3,5-bis(Trifluoromethyl)phenyl]methyl (1R,5S,6S)-6-{[(1H-1,2,3-benzotriazol-5-yl)formamido]methyl}-3-azabicyclo[3.1.0]hexane-3-carboxylate
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About This Item
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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
O=C(N1C[C@]2([H])[C@@H](CNC(C3=CC=C(NN=N4)C4=C3)=O)[C@]2([H])C1)OCC5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5
生化／生理作用
BI-2545 is a PF-8380 structure analog with improved autotaxin (ATX; ENPP2) inhibitory potency (human/rat ATX IC50 = 2.2/3.4 nM, IC50 = 29/96 nM using human/rat whole blood (WB); human ATX/rat ATX/rat WB IC50 = 6.5/13/307 nM with PF-8380), in vivo pharmacokinetic profile, oral availability, and lysophosphatidic acid (LPA)-lowering efficacy (BI-2545 Cmax/AUC/T1/2/Max 18:2 LPA reduction = 140 nM/675 nM•h/3.4 h/90.4% post 10 mg/kg p.o. in rats vs. 60.3 nM/342 nM•h/2.5 h/32.2% with PF-8380). BI-2545 exhibits no hERG inhibitory activity (IC50 >10 μM vs. 480 nM with PF-8380) and displays significant cross-reactivity towards only 4 targets among a panel of 48 enzymes/receptors/transporters/channel proteins at a high concentration of 10 μM (55%, 80%, 66%, 61% inhibtion of 5-HT2a, L-type Calcium channel, Na+ channel site 2, and norepinephrine transporter, respectively).
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Christian A Kuttruff et al.
ACS medicinal chemistry letters, 8(12), 1252-1257 (2017-12-21)
In an effort to find new therapeutic interventions addressing the unmet medical need of patients with idiopathic pulmonary fibrosis, we initiated a program to identify new autotaxin (ATX) inhibitors. Starting from a recently published compound (PF-8380), we identified several highly
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