Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&IC50 | P2Y1:0.06-0.3 μM(EC50) |
In vivo | Octreotide-treated groups show a significant reduction in the tumor volume when compared with saline group. Octreotide-PPSG (1.4 mg/kg, i.p.) shows greater antitumor effect than Octreotide-soln (100 μg/kg, i.p.). Octreotide-treatments results in significant inhibitory effect on the expression levels of SSTR2 and SSTR5 in primary HCC-bearing rats compared with the saline group. Octreotide-PPSG appears to inhibit the expression of SSTR2 and SSTR5 to a greater extent than that of Octreotide-soln treated group. A test dose of octreotide acetate significantly decreases the serum gastrin level to approximately one third of the baseline in 2 hr and the effect lasted approximately for 6 hr. On day 21, treatment with sustained-release formulation of octreotide acetatea (5 mg intramuscular, q 4 wk) is initiated. |
別名 | BMS-646786 |
分子量 | 445.43 |
分子式 | C23H22F3N3O3 |
CAS No. | 870544-59-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/mL (44.9 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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BPTU 870544-59-5 GPCR/G Protein Neuroscience P2Y Receptor antithrombotic thrombosis BMS-646786 BMS646786 inhibit BMS 646786 Inhibitor inhibitor