Description
EXP-3174 is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver. EXP-3174 is a potent angiotensin II receptor, type 1 (AT1) antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation. When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan. However, the metabolite has very low oral bioavailability.
EXP-3174 is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver. EXP-3174 is a potent angiotensin II receptor, type 1 (AT1) antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation. When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan. However, the metabolite has very low oral bioavailability.
Alternate Name/Synonyms: 1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1H-imidazole-5-carboxylic acid; Losartan carboxylic acid
Appearance: Off-white solid
Formulation: N/A
CAS Number: 124750-92-1
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₂₂H₂₁ClN₆O₂
Molecular Weight: 436.9
Cell-Permeable?: Yes
Purity: ≥98% by HPLC
Solubilities: DMSO (>20 mg/ml)
Handling: Protect from air and light
Country of Origin: USA
Tag Line: A physiologically active metabolite of losartan
MDL Number: N/A
PubChem CID: 108185
SMILES: CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)O)Cl
InChi: InChI=1S/C22H21ClN6O2/c1-2-3-8-18-24-20(23)19(22(30)31)29(18)13-14-9-11-15(12-10-14)16-6-4-5-7-17(16)21-25-27-28-26-21/h4-7,9-12H,2-3,8,13H2,1H3,(H,30,31)(H,25,26,27,28)
InChi Key: ZEUXAIYYDDCIRX-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |