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BI-2545
CAS No. 2162961-71-7
BI-2545( BI2545 | BI 2545 )
Catalog No. M13450 CAS No. 2162961-71-7
BI-2545 is a novel potent, selective, orally available Autotaxin inhibitor with IC50 of 2.1 and 3.4 nM for huamn and rat ATX, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
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Biological Information
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Product NameBI-2545
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NoteResearch use only, not for human use.
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Brief DescriptionBI-2545 is a novel potent, selective, orally available Autotaxin inhibitor with IC50 of 2.1 and 3.4 nM for huamn and rat ATX, respectively.
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DescriptionBI-2545 is a novel potent, selective, orally available Autotaxin inhibitor with IC50 of 2.1 and 3.4 nM for huamn and rat ATX, respectively; displays good potency in the LPA and rat whole blood assay (IC50=29 nM); shows substantial lowering of LPA in vivo, and excellent PK/Target Engagement relationship.
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In VitroBI-2545 displays good potency in the LPA and rat whole blood assay with IC50s of 29 nM and 96 nM, respectively.
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In VivoBI-2545 (10 mg/kg; p.o.) has high and sustained in vivo efficacy in reducing LPAs.BI-2545 (10 mg/kg; p.o.) has a half-life of t1/2=3.4 hours. Animal Model:Rat Dosage:10 mg/kg Administration:Oral administration Result:Reduces the sum of the plasma LPA species up to 90%.
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SynonymsBI2545 | BI 2545
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PathwayWnt/Notch/Hedgehog
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TargetAutotaxin
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RecptorAutotaxin
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Research Area——
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Indication——
Chemical Information
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CAS Number2162961-71-7
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Formula Weight527.427
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Molecular FormulaC23H19F6N5O3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 250 mg/mL (474.01 mM)
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SMILESO=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
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Chemical Name3,5-bis(trifluoromethyl)benzyl (1R,5S,6r)-6-((1H-benzo[d][1,2,3]triazole-5-carboxamido)methyl)-3-azabicyclo[3.1.0]hexane-3-carboxylate
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Christian A. Kuttruff, et al. ACS Med. Chem. Lett., 2017, 8 (12), pp 1252-1257. DOI: 10.1021/acsmedchemlett.7b00312
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