[CAS NO. 152918-26-8] AB-MECA
PRODUCTS SPECIFICATIONS [152918-26-8]
DESCRIPTION [152918-26-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 399.40 |
| Molecular Formula | C18H21N7O4 |
| SMILES | O[C@H]1[C@H](N2C=NC3=C(NCC4=CC=C(N)C=C4)N=CN=C23)O[C@H](C(NC)=O)[C@H]1O |
Summary
AB-MECA is a high affinity A 3 adenosine receptor agonist with a binding K i of 430.5 nM for human A 3 receptors in CHO cells. AB-MECA can enhance plasma histamine level [1] [2] [3] [4] .
IC50 & Target
|
Adenosine A 3 receptor |
In Vitro
AB-MECA (1, 10, 100 μM; 24 hours) shows dose-dependent cytotoxicity in human lung cancer cell line A549
[2]
.
[
125
I]AB-MECA has K
D
values for binding to A
3
receptors in transfected CHO cells and in RBL-2H3 cells are 1.48 and 3.61 nM, respectively
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay [2]
| Cell Line: | A549 cell |
| Concentration: | 1, 10, 100 μM |
| Incubation Time: | 24 hours |
| Result: | Shown dose-dependent cytotoxicity. |
In Vivo
AB-MECA (3 ug/kg; iv) enhances plasma histamine level in mouse
[4]
.
AB-MECA (0.3 mg/kg; iv) enhances antigen-induced bronchoconstriction in male albino guinea pigs, weighing 180-220 g
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Balb/c mice, weighing 18-25 g [4] |
| Dosage: | 3 ug/kg |
| Administration: | IV; single dose |
| Result: | Induced a 5.9-fold increase in histamine levels in murine plasma. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 55 mg/mL ( 137.71 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5038 mL | 12.5188 mL | 25.0376 mL |
| 5 mM | 0.5008 mL | 2.5038 mL | 5.0075 mL |
| 10 mM | 0.2504 mL | 1.2519 mL | 2.5038 mL |
References
- [1] L Yates, et al. Radioligand binding and functional responses of ligands for human recombinant adenosine A(3) receptors. Auton Autacoid Pharmacol. 2006 Apr;26(2):191-200.
- [2] Solanki, N. D., et al. In Vitro Evaluation Of Anti-Cancer Potential Of A3 Adenosine Receptor Agonist On A549 Human Lung Cancer Cell Line. Int J Pharm Pharm Sci ; 2019 Jun; 11(6): 106-108.
- [3] X D Ji, et al. A selective agonist affinity label for A3 adenosine receptors. Biochem Biophys Res Commun. 1994 Aug 30;203(1):570-6.
- [4] Endre G Mikus, et al. Interaction of SSR161421, a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo. Eur J Pharmacol. 2013 Jan 15;699(1-3):62-6.
- [5] Endre G Mikus, et al. Evaluation of SSR161421, a novel orally active adenosine A3 receptor antagonist on pharmacology models. Eur J Pharmacol. 2013 Jan 15;699(1-3):172-9.
