J-104132

CAT: 0804-HY-10383Size: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-10383Size:1 Each
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Description
J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) (HY-P71446) -induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications[1][3].
CAS Number
[198279-45-7]
UNSPSC
12352005
Target
Endothelin Receptor
Related Pathways
GPCR/G Protein
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Cardiovascular Disease; Metabolic Disease
Solubility
10 mM in DMSO
Smiles
O=C(O)[C@H]1[C@H](C(C(C[C@H](C)C(O)=O)=C2)=CC=C2OC)C3=NC(CCCC)=CC=C3[C@@H]1C4=CC=C5OCOC5=C4
Molecular Formula
C31H33NO7
Molecular Weight
531.60
References & Citations
[1]Nishikibe M, et al. Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist. J Pharmacol Exp Ther. 1999 Jun;289 (3) :1262-70.|[2]Kitada K, et al. Endothelin ETB receptor is involved in sex differences in the development of balloon injury-induced neointimal formation. J Pharmacol Exp Ther. 2011 Feb;336 (2) :533-9.|[3]Kanie N, et al. Effects of chronic administration of the novel endothelin antagonist J-104132 on endothelial dysfunction in streptozotocin-induced diabetic rat. Br J Pharmacol. 2002 Apr;135 (8) :1935-42.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ETA; ETB

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