BMS-986020 sodium
(Synonyms: AM152 sodium) 目录号 : GC38470
An LPA1 receptor antagonist
Cas No.:1380650-53-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BMS 986020 is an antagonist of lysophosphatidic acid receptor 1 (LPA1; Kb = 0.0067 ?M).1 It is selective for LPA1 over LPA3 in CHO cells expressing the human receptors (IC50s = 0.3 and >1 ?M, respectively).2 BMS 986020 also inhibits organic anion transporting polypeptide 1B1 (OATP1B1), OATP1B3, the bile salt export pump (BSEP), multidrug resistant protein 3 (MDR3), multidrug resistance-associated protein 3 (MRP3), and MRP4 (IC50s = 0.17, 0.57, 4.8, 7.5, 22, and 6.2 ?M, respectively).1 It reduces bleomycin-induced lung fibrosis in rats when administered at a dose of 30 mg/kg twice per day. BMS 986020 (225 and 500 mg/kg per day) decreases total biliary bile acid levels and induces bile duct hyperplasia, cholangitis, and cholestasis in monkeys.3 It decreases infarct volume and neurological deficits in a mouse model of ischemic stroke induced by transient middle cerebral artery occlusion (MCAO) when administered at a dose of 5 mg/kg.4
1.Cheng, P.T.W., Kaltenbach, R.F., III, Zhang, H., et al.Discovery of an oxycyclohexyl acid lysophosphatidic acid receptor 1 (LPA1) antagonist BMS-986278 for the treatment of pulmonary fibrotic diseasesJ. Med. Chem.64(21)15549-15581(2021) 2.Hutchinson, J.H., Seiders, T.J., Wang, B., et al.Polycyclic antagonists of lysophosphatidic acid receptors(2010) 3.Sivaraman, L., Gill, M., Nelson, D.M., et al.Structure dependence and species sensitivity of in vivo hepatobiliary toxicity with lysophosphatidic acid receptor 1 (LPA1) antagonistsToxicol. Appl. Pharmacol.115846(2021) 4.Gaire, B.P., Sapkota, A., and Choi, J.W.BMS-986020, a specific LPA1 antagonist, provides neuroprotection against ischemic stroke in miceAntioxidants (Basel)9(11)1097(2020)
| Cas No. | 1380650-53-2 | SDF | |
| 别名 | AM152 sodium | ||
| Canonical SMILES | O=C(C1(C2=CC=C(C3=CC=C(C4=C(NC(O[C@@H](C5=CC=CC=C5)C)=O)C(C)=NO4)C=C3)C=C2)CC1)[O-].[Na+] | ||
| 分子式 | C29H25N2NaO5 | 分子量 | 504.51 |
| 溶解度 | DMSO: 150 mg/mL (297.32 mM); Water: < 0.1 mg/mL (insoluble) | 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。 |
||
| 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 | 1.9821 mL | 9.9106 mL | 19.8212 mL |
| 5 mM | 0.3964 mL | 1.9821 mL | 3.9642 mL |
| 10 mM | 0.1982 mL | 0.9911 mL | 1.9821 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。