ELN-441958_product_DataBase

Bioactivity

ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse[1].

Target

Ki: 0.26 nM (native human bradykinin B1 receptor)

Invitro

ELN-441958 is selective for primate over rodent B1 receptors with a rank order potency (KB, nanomolar) of human (0.12 ± 0.02) ~ rhesus monkey (0.24 ± 0.01) > rat (1.5 ± 0.4) > mouse (14 ± 4)[1].ELN-441958 has good permeability and metabolic stability[1].

In Vivo

ELN-441958 (1-10 mg/kg; s.c.; once) dose-dependently reduces carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model[1].ELN-441958 (0-10 mg/kg; i.v. or p.o.) exhibits a favorable pharmacokinetic profile in the rat and rhesus monkey[1]. Animal Model:

Name

ELN-441958

CAS

913064-47-8

Formula

C29H29ClN4O2

Molar Mass

501.02

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Hawkinson JE, et al. Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958. J Pharmacol Exp Ther.2007 Aug;322(2):619-630.

PeptideDB

ELN-441958

CAS: 913064-47-8 F: C29H29ClN4O2 W: 501.02