BCRP-IN-1
目录号 : GC33099BCRP-IN-1 是一种乳腺癌耐药蛋白 (BCRP) 抑制剂,对 BCRP 外排转运蛋白的 IC50 为 0.6 μM。
Cas No.:1699720-85-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice[1]To determine pharmacokinetic profile of (S)-ML753286 and Ko143 in vivo, Sprague-Dawley rats are administered 2.0 mg/kg or 20 mg/kg (S)-ML753286 or 2.0 mg/kg or 50 mg/kg Ko143, formulated in 0.5% HPMC/0.2% Tween80, via iv or po, respectively. After administration of (S)-ML753286 or Ko143, blood is obtained from all animals at predose and at 0.083, 0.25, 0.5, 1, 4, 8, and 24 h postdose. Approximately 200 μL of whole blood is collected from the jugular vein catheter of each animal into tubes containing the anticoagulant dipotassium ethylenediaminetetraacetic acid (K2EDTA) and is further processed into plasma at approximately 4°C[1]. |
References: [1]. Li Y, et al. Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles. Bioorg Med Chem Lett. 2016 Jan 15;26(2):551-555. |
BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
BCRP-IN-1 (Compound A) shows the potency and a potent pharmacokinetic (PK) profile in rats (lower clearance [1.54 L/h/kg] and higher bioavailability [123%]). XL388 has moderate terminal elimination half-life with t1/2s of 0.9 h and 2.0 h for 2 mg/kg (iv) and 20 mg/kg (po) in rats, respectively[1].
[1]. Li Y, et al. Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles. Bioorg Med Chem Lett. 2016 Jan 15;26(2):551-555.
Cas No. | 1699720-85-8 | SDF | |
Canonical SMILES | COC1=CC=C2C(NC3=C2C[C@]4([H])N(C([C@H](C)NC4=O)=O)[C@H]3CC(C)C)=C1 | ||
分子式 | C20H25N3O3 | 分子量 | 355.43 |
溶解度 | DMSO : ≥ 50 mg/mL (140.67 mM) | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.8135 mL | 14.0675 mL | 28.1349 mL |
5 mM | 0.5627 mL | 2.8135 mL | 5.627 mL |
10 mM | 0.2813 mL | 1.4067 mL | 2.8135 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。