R 8231
For research use only. We do not sell to patients.
- CAS No.: 50648-52-7
- Formula: C13H11BrN2O4S
- Molecular Weight:371.21
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
R 8231 (at a maximum concentration of 0.5 mM) does not significantly inhibit alkaline phosphatase activity in fixed HeLa cells, indicating that alkaline phosphatase derived from HeLa cells is insensitive to R 8231[1].
After treatment of rat tissue sections with R 8231 (0.1 mM; 37°C; pre-incubation for 1 h) and subsequent transfer to an inhibitor-free reaction solution, the alkaline phosphatase reaction product does not decrease, indicating that the inhibitory effect of R 8231 is reversible[1].
R 8231 (1 μM) potently inhibits purified alkaline phosphatase isozymes derived from human liver, bone, kidney and spleen via an uncompetitive mechanism. Under the tested conditions, the maximum inhibition rate of R 8231 against human liver alkaline phosphatase reaches 68%, while it exerts weak effects on alkaline phosphatase isozymes derived from human intestine and placenta[2].
R 8231 (10-100 μM; 6 days) almost completely inhibits the activity of bone alkaline phosphatase in rat embryos, but does not inhibit the growth of rat embryonic femur explants under in vitro culture conditions[3].
R 8231 (0.5 mM) inhibits the interference of non-specific alkaline phosphatase in homogenates of secretory-stage enamel organs from Sprague-Dawley rats, and thus is used for the specific detection of Ca2+-stimulated ATPase activity with an optimal pH of 8.2. In standard enzyme activity assays, the reaction duration ranges from 2-15 min; in ATP metabolism time-course assays with a maximum duration of 30 min, the reaction in the system containing R 8231 proceeds slightly slower, and the production of AMP and adenosine is reduced[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
-
CAS No. 50648-52-7
-
Molecular Weight 371.21
-
Formula C13H11BrN2O4S
-
SMILES
O=C(C(O)=O)O.BrC1=CC=CC(C2N=C3SC=CN3C2)=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[1]. Borgers M. The cytochemical application of new potent inhibitors of alkaline phosphatases. J Histochem Cytochem. 1973;21(9):812-824. [Content Brief]
[2]. Van Belle H, et al. Alkaline phosphatase. I. Kinetics and inhibition by levamisole of purified isoenzymes from humans. Clinical chemistry. 1976 Jul;22(7):972-6. [Content Brief]
[3]. Reynolds JJ, et al. Comparison of the inhibition of avian and mammalian bone alkaline phosphatases by levamisole and compound R8231. Experientia. 1977;33(2):154-155. [Content Brief]
[4]. Mörnstad H, et al. Calcium-stimulated ATPase activity in homogenates of the secretory enamel organ in the rat. Scandinavian journal of dental research. 1978 Jan;86(1):1-11. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- R 8231
- 50648-52-7
- R8231
- R-8231
- Phosphatase
- human intestinal alkaline phosphatase
- human non-intestinal alkaline phosphatase isoenzymes
- HeLa cells
- mammalian bone alkaline phosphatase
- embryonic rat femur
- bone metabolism
- alkaline phosphatase
- chick bone alkaline phosphatase
- rat kidney proximal convoluted tubule brush border alkaline phosphatase
- chick embryonic femur explant
- Inhibitor
- inhibitor
- inhibit