BPTU
Based on 2 publication(s) in Google Scholar
BPTU (BMS-646786) is a non-nucleotide P2Y1 receptor allosteric antagonist with antithrombotic activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.67%
- CAS. Nr.: 870544-59-5
- Formel: C23H22F3N3O3
- Molecular Weight:445.43
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) BPTU
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Biologische Aktivität
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P2Y1 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
11 μM
Compound: 1
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Antiplatelet activity in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation in presence of 10 uM ADP
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation in presence of 10 uM ADP
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[PMID: 24767843] |
| Platelet | IC50 |
2.1 μM
Compound: 1
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Antiplatelet activity against platelet (unknown origin) assessed as inhibition of ADP-induced platelet aggregation
Antiplatelet activity against platelet (unknown origin) assessed as inhibition of ADP-induced platelet aggregation
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[PMID: 23602442] |
| Platelet | IC50 |
2.1 μM
Compound: 16
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Inhibition of ADP-induced platelet aggregation in human platelet rich plasma
Inhibition of ADP-induced platelet aggregation in human platelet rich plasma
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[PMID: 23368907] |
BPTU blocks the supramaximal fast inhibitory junction potentials (fIJP) in a concentration-dependent manner both in the rat and mouse colon. The EC50 of BPTU is approximately 0.3 μM and 0.06 μM for the rat and mouse colon, respectively. In the rat colon, addition of the P2Y agonist ADPβS at 10 μM significantly reduces spontaneous contractions to a 43.2±13.4% (N=5) (P=0.0002), and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.3±5.1%). Similar results are obtained in the murine colon where ADPβS at 10 μM reduces the area under the curve (AUC) of contractions to a 15.8±5.1% (N=4) (P<0.0001) and its effect is reversed with BPTU at 3 μM (82.7±3.6%). Addition of MRS2365, a selective P2Y1 agonist, at a concentration of 5 μM significantly reduces spontaneous contractions to a 21.2±4.8% (N=5) (P=0.0002) in the murine colon, and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.1±3.8%). The blockage of the MRS2365-induced response by BPTU at 3 μM also occurs in control conditions (N=5) (10.2±5.5% vs. 86.7±5.0%)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 870544-59-5
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Appearance Solid
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Molecular Weight 445.43
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Formel C23H22F3N3O3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(OC(F)(F)F)C=C1)NC2=CC=CN=C2OC3=CC=CC=C3C(C)(C)C
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Synonyms
BMS-646786
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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bioRxiv
2026 May 14:2026.05.11.724407. PMID: 42182450
Lösungsmittel & Löslichkeit
DMSO : ≥ 33.3 mg/mL (74.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Electrophysiological experiments are performed with colonic rat and mouse strips. Inhibitory junction potentials (IJP) are elicited by electrical field stimulation (EFS) using two silver chloride plates placed 1.5 cm apart perpendicular to the longitudinal axis of the preparation. The protocol consists of single pulse trains of EFS (0.4 ms pulse duration) at increasing voltages (8, 12, 16, 20, 24, 28, 32, 36, 40 V). The voltage responsible for the supramaximal response is used to elicit single pulses during incubation with BPTU at increasing concentrations (1×10-8 M, 1×10-7 M, 3×10-7 M, 1×10-6 M and 3×10-6 M). Another train of single pulses at increasing voltages is elicited after the highest dose of BPTU. The amplitude of the IJP (mV) is measured considering it as the difference between the maximal hyperpolarization and the resting membrane potential (RMP)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice are given BPTU intraperitoneally at doses of 3.15 mg of boron per kg body weight. Injection volumes range from 0.25 to 0.5 mL for both intravenous and intraperitoneal administrations. Six mice are not given any drug to allow measurement of boron background levels. Animals are killed with carbon dioxide 0.2, 0.4, 1, 2, 4, 24 and 48 h after drug administration and samples are taken from tumor, blood, skin, muscle, brain, kidneys and liver. Tumor tissue from mice bearing B16.013 tumor is checked by eye for the absence of pigmentation. BPTU is also given in a multiple dose scheme. Every 2 h 0.4 to 0.5 mL of the above-mentioned BPTU solution is given intraperitoneally (4×3.15 mg/kg boron). Twenty-four hours after the last administration, the animals are sacrificed and samples are taken[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Noemí Mañé, et al. BPTU, an allosteric antagonist of P2Y1 receptor, blocks nerve mediated inhibitory neuromuscular responses in the gastrointestinal tract of rodents. Neuropharmacology. 2016 Nov;110(Pt A):376-385. [Content Brief]
[2]. Dandan Zhang, et al. Two disparate ligand binding sites in the human P2Y1 receptor. Nature. 2015 Apr 16; 520(7547): 317–321. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2450 mL | 11.2251 mL | 22.4502 mL | 56.1255 mL |
| 5 mM | 0.4490 mL | 2.2450 mL | 4.4900 mL | 11.2251 mL | |
| 10 mM | 0.2245 mL | 1.1225 mL | 2.2450 mL | 5.6126 mL | |
| 15 mM | 0.1497 mL | 0.7483 mL | 1.4967 mL | 3.7417 mL | |
| 20 mM | 0.1123 mL | 0.5613 mL | 1.1225 mL | 2.8063 mL | |
| 25 mM | 0.0898 mL | 0.4490 mL | 0.8980 mL | 2.2450 mL | |
| 30 mM | 0.0748 mL | 0.3742 mL | 0.7483 mL | 1.8709 mL | |
| 40 mM | 0.0561 mL | 0.2806 mL | 0.5613 mL | 1.4031 mL | |
| 50 mM | 0.0449 mL | 0.2245 mL | 0.4490 mL | 1.1225 mL | |
| 60 mM | 0.0374 mL | 0.1871 mL | 0.3742 mL | 0.9354 mL |
BPTU Related Classifications
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