BIBB 515|cas:156635-05-1|西域试剂

BIBB 515,99.44%

产品编号：Bellancom-116175| CAS NO：156635-05-1| 分子式：C₂₂H₂₁ClN₂O₂| 分子量：380.87

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-116175	￥700.00	杭州北京（现货）
Bellancom-116175	￥2100.00	杭州北京（现货）
Bellancom-116175	￥3600.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

BIBB 515

产品介绍

BIBB 515 是一种有效的，选择性的和口服活性的 2,3-氧化角鲨烯环化酶 (OSC) 抑制剂，在大鼠和小鼠中的 ED₅₀ 值分别为 0.2-0.5 mg/kg 和 0.36-33.3 mg/kg (1-5 小时)。BIBB 515 主要通过抑制低密度脂蛋白 (LDL) 的产生来发挥降脂作用。

生物活性

BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED₅₀ values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL).

体外研究

Sterol synthesis, 2,3-oxidosqualene cyclase activity, HMGCoA reductase activity, and the specificity of BIBB 51 5 versus 2,3-oxidosqualene cyclase are measured in intact HepG2 cells or cell homogenates.Concentration-dependent inhibition of cholesterol biosynthesis by BIBB 515 as monitored by [¹⁴C]-acetate incorporation into digitonin precipitable sterols could be demonstrated in HepG2 cells (ED₅₀ = 4.11 nM). A similar inhibition of OSC activity (ED₅₀= 8.69 nM) is seen in HepC2 cell homogenates. No inhibition of HMGCoA reductasc could be measured in HepG2 cell homogenates at concentrations of BIBB 515 up to 1 and 10 μM.

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

体内研究

BIBB 515 (16.0-148.2 mg/ kg; oral administration; daily; for 40 days; male golden Syrian hyperlipemic hamsters) treatment shows dose-dependent lipid-lowering activity in normolipemic hamsters (-19% for total cholesterol and -32% for VLDL + LDL cholesterol) and in hyperlipemic hamsters (-25% for total cholesterol and -59% for LDL-cholesterol).

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

Animal Model:	Male golden Syrian hyperlipemic hamsters (~100 g)
Dosage:	16.0 mg/ kg, 49.7 mg/ kg, and 148.2 mg/ kg
Administration:	Oral administration; daily; for 40 days
Result:	Dose-dependent lipid-lowering activity was seen in normolipemic hamsters after 11 days treatment (-19% for total cholesterol and -32% for VLDL + LDL cholesterol at 55 mg/kg/day) and in hyperlipemic hamsters after 25 days (-25% for total cholesterol and -59% for LDL-cholesterol at 148 mg/kg/day).

体内研究

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

Animal Model:	Male golden Syrian hyperlipemic hamsters (~100 g)
Dosage:	16.0 mg/ kg, 49.7 mg/ kg, and 148.2 mg/ kg
Administration:	Oral administration; daily; for 40 days
Result:	Dose-dependent lipid-lowering activity was seen in normolipemic hamsters after 11 days treatment (-19% for total cholesterol and -32% for VLDL + LDL cholesterol at 55 mg/kg/day) and in hyperlipemic hamsters after 25 days (-25% for total cholesterol and -59% for LDL-cholesterol at 148 mg/kg/day).

性状

Solid

溶解性数据

In Vitro:

DMSO : 2.5 mg/mL (6.56 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6256 mL	13.1278 mL	26.2557 mL
5 mM	0.5251 mL	2.6256 mL	5.2511 mL
10 mM	---	---	---

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。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式