Relacatib SB-462795|cas:362505-84-8|西域试剂

Relacatib SB-462795,98.26%

产品编号：Bellancom-10294| CAS NO：362505-84-8| 分子式：C₂₇H₃₂N₄O₆S| 分子量：540.63

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-10294		￥11500.00	杭州北京（现货）

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Relacatib SB-462795

产品介绍

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。

生物活性

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with K_i values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC₅₀ values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Cynomolgus monkey
Dosage:	12 mg/kg
Administration:	Subcutaneous injection; single dose; blood sample is drawn 1.5, 4, 24, 48, and 72 h post dose administration
Result:	Was sufficiently high to significantly suppress bone resorption from 1.5 to 72 h post dosing.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Cynomolgus monkey
Dosage:	12 mg/kg
Administration:	Subcutaneous injection; single dose; blood sample is drawn 1.5, 4, 24, 48, and 72 h post dose administration
Result:	Was sufficiently high to significantly suppress bone resorption from 1.5 to 72 h post dosing.

性状

Solid

溶解性数据

In Vitro:

DMSO : 40 mg/mL (73.99 mM; ultrasonic and warming and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8497 mL	9.2485 mL	18.4969 mL
5 mM	0.3699 mL	1.8497 mL	3.6994 mL
10 mM	0.1850 mL	0.9248 mL	1.8497 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

1.

SSB-462795 is prepared as a nanosuspension containing 1.5% Methylcellulose and 2.0% sodium lauryl sulfate.
2.

SB-462795 (12 mg/kg) or vehicle is in 70% aqueous PEG400(1 ml/kg).