BAY-545
Based on 1 Customer Validation
BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.79%
- CAS No.: 1699717-32-2
- 화학식: C18H22F3N3O4S
- 분자량:433.45
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
All Adenosine Receptor Isoforms
More
Biological Activity
IC50: 59 nM (A2B adenosine receptor), 66 nM (Human A2B adenosine receptor), 400 nM (Mouse A2B adenosine receptor), 280 nM (Rat A2B adenosine receptor), 1300 nM (Human A1 adenosine receptor), 820 nM (Human A2A adenosine receptor), 470 nM (Mouse A2A adenosine receptor) and 750 nM (Rat A2A adenosine receptor)[1]
Ki: 97 nM (A2B adenosine receptor)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.28 μM
Compound: 8; BAY-545
|
Antagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
Antagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
|
[PMID: 30576906] |
| CHO | IC50 |
66 nM
Compound: 8; BAY-545
|
Antagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
Antagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
|
[PMID: 30576906] |
| CHO | IC50 |
>6.7 μM
Compound: 8; BAY-545
|
Antagonist activity at recombinant mouse A3 adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
Antagonist activity at recombinant mouse A3 adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
|
[PMID: 30576906] |
| CHO | IC50 |
0.75 μM
Compound: 8; BAY-545
|
Antagonist activity at recombinant rat A2A adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
Antagonist activity at recombinant rat A2A adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
|
[PMID: 30576906] |
| CHO | IC50 |
1.3 μM
Compound: 8; BAY-545
|
Antagonist activity at recombinant human A1 adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
Antagonist activity at recombinant human A1 adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
|
[PMID: 30576906] |
| CHO | IC50 |
0.82 μM
Compound: 8; BAY-545
|
Antagonist activity at recombinant human A2A adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
Antagonist activity at recombinant human A2A adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
|
[PMID: 30576906] |
| CHO | IC50 |
0.47 μM
Compound: 8; BAY-545
|
Antagonist activity at recombinant mouse A2A adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
Antagonist activity at recombinant mouse A2A adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
|
[PMID: 30576906] |
| HEK293 | IC50 |
59 nM
Compound: 8; BAY-545
|
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
|
[PMID: 30576906] |
BAY-545 is selective at A2B adenosine receptor over A1, A2A, and A3 adenosine receptor, with IC50s of 1300 nM (Human A1 adenosine receptor), 820 nM (Human A2A adenosine receptor), 470 nM (Mouse A2A adenosine receptor) and 750 nM (Rat A2A adenosine receptor)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1699717-32-2
-
Appearance Solid
-
분자량 433.45
-
화학식 C18H22F3N3O4S
-
Color White to off-white
-
SMILES
CCN1C(N(CCC(F)(F)F)C2=C(C(C)=C(C(N3CCC(O)CC3)=O)S2)C1=O)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : ≥ 150 mg/mL (346.06 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.77 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.77 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
순도&문서
-
Data Sheet (276 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
Handling Instructions (2659 KB)
References
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 | 2.3071 mL | 11.5354 mL | 23.0707 mL | 57.6768 mL |
| 5 mM | 0.4614 mL | 2.3071 mL | 4.6141 mL | 11.5354 mL | |
| 10 mM | 0.2307 mL | 1.1535 mL | 2.3071 mL | 5.7677 mL | |
| 15 mM | 0.1538 mL | 0.7690 mL | 1.5380 mL | 3.8451 mL | |
| 20 mM | 0.1154 mL | 0.5768 mL | 1.1535 mL | 2.8838 mL | |
| 25 mM | 0.0923 mL | 0.4614 mL | 0.9228 mL | 2.3071 mL | |
| 30 mM | 0.0769 mL | 0.3845 mL | 0.7690 mL | 1.9226 mL | |
| 40 mM | 0.0577 mL | 0.2884 mL | 0.5768 mL | 1.4419 mL | |
| 50 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL | 1.1535 mL | |
| 60 mM | 0.0385 mL | 0.1923 mL | 0.3845 mL | 0.9613 mL | |
| 80 mM | 0.0288 mL | 0.1442 mL | 0.2884 mL | 0.7210 mL | |
| 100 mM | 0.0231 mL | 0.1154 mL | 0.2307 mL | 0.5768 mL |
BAY-545 Related Classifications
HY-111767 Related Classifications
Powered by Bioz