LAS101057
Based on 1 publication(s) in Google Scholar
LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 925676-48-8
- Formula: C18H14FN5O
- Molecular Weight:335.34
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) LAS101057
MoreAll Adenosine Receptor Isoforms
More
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
512 nM
Compound: 17, LAS101057
|
Antagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
Antagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
|
[PMID: 24900298] |
| HEK293 | IC50 |
120 nM
Compound: 17, LAS101057
|
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
|
[PMID: 24900298] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 925676-48-8
-
Appearance Solid
-
Molecular Weight 335.34
-
Formula C18H14FN5O
-
Color White to off-white
-
SMILES
FC1=CN=CC=C1C(N=CC(NC(C2CC2)=O)=N3)=C3C4=CC=CN=C4
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Acta Pharm Sin B
Bone-derived MSCs encapsulated in alginate hydrogel prevent collagen-induced arthritis in mice through the activation of adenosine A2A/2B receptors in tolerogenic dendritic cells. [Abstract]2023 Jun;13(6):2778-2794. PMID: 37425054
Solvent & Solubility
DMSO : ≥ 125 mg/mL (372.76 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.08 mg/mL (6.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
-
-
-
-
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Purity & Documentation
-
Data Sheet (273 KB)
-
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)
-
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9820 mL | 14.9102 mL | 29.8205 mL | 74.5512 mL |
| 5 mM | 0.5964 mL | 2.9820 mL | 5.9641 mL | 14.9102 mL | |
| 10 mM | 0.2982 mL | 1.4910 mL | 2.9820 mL | 7.4551 mL | |
| 15 mM | 0.1988 mL | 0.9940 mL | 1.9880 mL | 4.9701 mL | |
| 20 mM | 0.1491 mL | 0.7455 mL | 1.4910 mL | 3.7276 mL | |
| 25 mM | 0.1193 mL | 0.5964 mL | 1.1928 mL | 2.9820 mL | |
| 30 mM | 0.0994 mL | 0.4970 mL | 0.9940 mL | 2.4850 mL | |
| 40 mM | 0.0746 mL | 0.3728 mL | 0.7455 mL | 1.8638 mL | |
| 50 mM | 0.0596 mL | 0.2982 mL | 0.5964 mL | 1.4910 mL | |
| 60 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2425 mL | |
| 80 mM | 0.0373 mL | 0.1864 mL | 0.3728 mL | 0.9319 mL | |
| 100 mM | 0.0298 mL | 0.1491 mL | 0.2982 mL | 0.7455 mL |