|(R)-3-(4-氰基-3-(3-((1-(2,3-二氢-1H-茚-2-基)-2-甲基丙-2-基)氨基)-2-羟基丙氧基 )苯基)丙酸|CsnPharm

CAS No.: 351490-27-2

SB-423562 Catalog No. CSN24273

Synonyms: NPSP-795

SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Parathyroid hormone (PTH) plays an essential role in calcium homeostasis by regulating bone resorption, renal calcium excretion, and intestinal calcium absorption. SB-423562 is a novel, short-acting antagonist for calcium-sensing receptor (CaR) that can induce transient PTH release from parathyroid gland. SB-423562 showed a potent in vitro inhibition of CaR-mediated signaling in HEK-293 cells transfected with human CaR (IC50 = 73nM). In rats, SB-423562 was cleared rapidly (89 mL/min/kg) following the i.v. administration and exhibited a short half-life of 0.23h. In preclinical animal models, systemic treatment of SB-423562 following oral administration did not sufficiently induce PTH release due to the poor intestinal absorption and high hepatic extraction of SB-423562. The administration of SB-423557, the ethyl ester precursor of SB-423562, at 15 and 50mg/kg dose-dependently and transiently increased the circulating level of endogenous PTH in rats as compared to the vehicle-treated controls. SB-423557 treatment also resulted in a transient and significant dose-dependent rise (∼10%) in serum Ca²⁺ at 1 and 2 h post-dose. The transient upregulation of plasma PTH was also observed in dogs (25mg/kg) and monkeys (50mg/kg) following oral administration of SB-423557. The oral administration of SB-423557 (50mg/kg) in ovariectomized rats for 12 weeks significantly increased the bone mineral density (BMD) in lumbar spine, the trabecular BMD of proximal tibia and the endocortical bone formation rate of distal tibia as compared with the controls^[2].
动物研究
剂量
Rat: 5 mg/kg - 50 mg/kg^[1] (p.o.)

给药途径
p.o.

动物药代数据
Animal Rats^[1]
Administration i.v.
CL 89 ml/min/kg
T_1/2 0.23 h
V_d 0.8 L/kg
参考文献

[1] Kumar S, Matheny CJ, et al. An orally active calcium-sensing receptor antagonist that transiently increases plasma concentrations of PTH and stimulates bone formation. Bone. 2010 Feb;46(2):534-42.
[2] Kumar S, Matheny CJ, Hoffman SJ, Marquis RW, Schultz M, Liang X, Vasko JA, Stroup GB, Vaden VR, Haley H, Fox J, DelMar EG, Nemeth EF, Lago AM, Callahan JF, Bhatnagar P, Huffman WF, Gowen M, Yi B, Danoff TM, Fitzpatrick LA. An orally active calcium-sensing receptor antagonist that transiently increases plasma concentrations of PTH and stimulates bone formation. Bone. 2010 Feb;46(2):534-42.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2907 mL
- 11.4536 mL
- 22.9072 mL
- 5 mM
- 0.4581 mL
- 2.2907 mL
- 4.5814 mL
- 10 mM
- 0.2291 mL
- 1.1454 mL
- 2.2907 mL

技术信息

CAS号

351490-27-2

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H32N2O4

运输

蓝冰

分子量

436.54

别名

NPSP-795

溶解度

DMSO	17.5 mg/mL (40.1 mM)
Water	22.5 mg/mL (51.5 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

SB-423562 Catalog No. CSN24273

靶点选择性

请登录您的专属账户

确认信息