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Relacatib

CAS No. : 362505-84-8

MCE 站：Relacatib

产品活性：Relacatib (SB-462795) 是一种新的，有效的口服活性的人组织蛋白酶 K, L 和 V (cathepsins K, L, V) 的抑制剂，其K_i 值分别为 41, 68 和 53 pM。Relacatib 原位抑制人破骨细胞内源性组织蛋白酶 K 和人破骨细胞介导的骨吸收，IC₅₀ 值分别为 45 nM 和 70 nM。Relacatib 对体外人体组织骨吸收的抑制作用，以及对食蟹猴体内骨吸收有抑制作用。

研究领域：Metabolic Enzyme/Protease

作用靶点：Cathepsin

In Vitro: Relacatib are incubated with human osteoclastoma-derived osteoclasts seeded onto bovine cortical bone slices in vitro biological activity, it shows inhibitory potency with K_i values of 0.041 nM, 0.068 nM,0.063 nM,1.6 nM,and 13 nM against human cathepsin K, cathepsin L, cathepsin V, cathepsin S and cathepsin B, respectively in the assay.
Relacatib is against Monkey cathepsin K, cathepsin L,cathepsin V and cathepsin B with K_i values of 0.041 nM, 0.28 nM, 0.72 nM and 11nM, respectively. Relacatib is against mouse cathepsin L and rat cathepsin L with K_i values of 0.20 nM and 0.17 nM, respectively.

In Vivo: Relacatib (1-2 mg/kg 0.5 h intravenous infusion; 2-4 mg/kg oral bolus gavage) exhibits T_1/2, CL or V_dss with 109 mins, 19.5 mL/min/kg, or 1.86 L/kg in male Sprague-Dawley rats and 168 mins, 11.7 mL/min/kg, and 1.79 L/kg in monkeys, respectively in a PK iv/po crossover studies. The oral bioavailability of Relacatib is 28% in the monkey and 89.4% in the rats.
SB-462795 (subcutaneous injection; 12 mg/kg; blood sample is drawn 1.5, 4, 24, 48, and 72 h post dose administration) significantly inhibits resorption as assessed by two markers of bone resorption,the N- (NTx) and C-telopeptides (CTx) of type I collagen measured in serum. SB-462795 does not exhibit difference of serum osteocalcin (a biomarker of osteoblast activity) between SB-462795 and vehicle treated animalsexcept for the 48 h time point where a significant reduction (42% lower than baseline vs. 18% lower than baseline with vehicle treatment).

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