Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2086 |
ELN-441958
ELN 441958 |
Bradykinin Receptor | GPCR/G Protein |
ELN-441958是一种B1受体拮抗剂,能够抑制B1激动剂配体[3H] DAKD 与IMR-90细胞结合(Ki:0.26 nM),相较于B2受体,它对B1受体的抑制作用具有更高的选择性,且比抑制μ阿片受体选择性高500多倍,比抑制δ阿片受体选择性高2000多倍。 | |||
T68356 | AM-3189 | ||
AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavai... |