ELN-441958,913064-47-8

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ELN-441958

CAS No. : 913064-47-8

MCE 国际站：ELN-441958

产品活性：ELN-441958 是一种有效的、中性的、竞争性的和选择性的缓激肽 B₁ 受体 (bradykinin B₁ receptor) 拮抗剂，K_i 值为 0.26 nM。ELN-441958 具有较高的口服生物利用度，在小鼠中 CNS 透过性低。

研究领域：GPCR/G Protein

作用靶点：Bradykinin Receptor

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

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.
ELN-441958 (0-10 mg/kg; i.v. or p.o.) exhibits a favorable pharmacokinetic profile in the rat and rhesus monkey.

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