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BPTU

Catalog No. T4132   CAS 870544-59-5
Synonyms: BMS-646786

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.

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BPTU Chemical Structure
BPTU, CAS 870544-59-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
2 mg In stock $ 45.00
5 mg In stock $ 66.00
10 mg In stock $ 118.00
25 mg In stock $ 251.00
50 mg In stock $ 433.00
100 mg In stock $ 642.00
1 mL * 10 mM (in DMSO) In stock $ 66.00
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Purity: 99.89%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&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.
Synonyms BMS-646786
Molecular Weight 445.43
Formula C23H22F3N3O3
CAS No. 870544-59-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mM

TargetMolReferences and Literature

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.

TargetMolCitations

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.

Related compound libraries

This product is contained In the following compound libraries:
Covalent Inhibitor Library Bioactive Compound Library Inhibitor Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Fluorochemical Library Anti-Cancer Compound Library GPCR Compound Library NO PAINS Compound Library

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Keywords

BPTU 870544-59-5 GPCR/G Protein Neuroscience P2Y Receptor antithrombotic thrombosis BMS-646786 BMS646786 inhibit BMS 646786 Inhibitor inhibitor

 

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