ELN 441958 is a novel bradykinin B1 Receptor antagonist. ELN441958 competitively inhibited the binding of the B(1) agonist ligand [(3)H]desArg(10)-kallidin ([(3)H]DAKD) to IMR-90 human fibroblast membranes with high affinity (K(i) = 0.26 +/- 0.02 nM). ELN441958 potently antagonized DAKD (but not bradykinin)-induced calcium mobilization in IMR-90 cells, indicating that it is highly selective for B(1) over B(2) receptors. Antagonism of agonist-induced calcium responses at B(1) receptors from different species indicated that ELN441958 is selective for primate over rodent B(1) receptors with a rank order potency (K(B), nanomolar) of human (0.12 +/- 0.02) approximately rhesus monkey (0.24 +/- 0.01) > rat (1.5 +/- 0.4) > mouse (14 +/- 4).

 

Brand: BCM

 

Solubility: Soluble in DMSO. Insoluble in Water and Ethanol.

 

InChi Key: ARYQHSWJGHCGJS-UHFFFAOYSA-N

 

Attribute
[Chem Name]	7-Chloro-2-[3-(9-pyridin-4-yl-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl]-3H-isoindol-1-one
[Synonym]	ELN441958; ELN 441958; ELN-441958
[CAS No.]	913064-47-8
[EINECS]	604-604-1
[MDL No.]	MFCD27665467
[Formula]	C29H29ClN4O2
[Molecular]	501.02
[Form]	Powder

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