| Description | BPTU (BMS-646786) is an allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM). Non-nucleotide ligand. Binds receptor outside of the helical bundle. Blocks inhibition of spontaneous contraction of rat and mouse colon induced by electrical field stimulation, nicotine and P2Y agonists. Antithrombotic; reduces platelet aggregation. |
| In vivo | Octreotide处理组与生理盐水组相比显著降低了肿瘤体积。Octreotide-PPSG (1.4 mg/kg, i.p.) 的抗肿瘤效果比Octreotide-soln (100 μg/kg, i.p.) 更为显著。Octreotide治疗显著抑制了携带原发性HCC的大鼠SSTR2和SSTR5的表达水平。相较于Octreotide-soln处理组，Octreotide-PPSG对SSTR2和SSTR5表达的抑制作用更强。 Octreotide Acetate 盐的测试剂量在2小时内显著降低血清胃泌素水平至基线的约三分之一，且效果持续约6小时。在第21天，开始使用持续释放配方的 Octreotide Acetate 盐(5 mg肌肉注射, 每4周一次)进行治疗。 |
| Target activity | P2Y1:0.06-0.3 μM(EC50) |
| Synonyms | BMS-646786 |
| molecular weight | 445.43 |
| Molecular formula | C23H22F3N3O3 |
| CAS | 870544-59-5 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 20 mg/mL (44.9 mM), Sonication is recommended. |
| References | 1. Abrahamsen B, et al. Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J Neurosci. 2013 Jan 16;33(3):1068-87. 2. Zhao T V, Li Y, Liu X, et al. ATP release drives heightened immune responses associated with hypertension[J]. Science immunology. 2019, 4(36): eaau6426. |
| Citations | 1. Zhao T V, Li Y, Liu X, et al. ATP release drives heightened immune responses associated with hypertension. Science immunology. 2019, 4(36): eaau6426. |