RX-RA 85
RX-RA 85 is an orally active phosphodiesterase modulator that exerts antiplatelet and antitumor effects by elevating intracellular cAMP levels, inhibiting platelet and tumor cell PDE activity, and modulating cytoskeletal organization. RX-RA 85 can be used in studies of rat breast cancer and metastatic tumors.
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- CAS No.: 77749-81-6
- Formule: C22H27N7OS2
- Masse moléculaire:469.63
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Activité biologique
Description
RX-RA 85 is an orally active phosphodiesterase modulator that exerts antiplatelet and antitumor effects by elevating intracellular cAMP levels, inhibiting platelet and tumor cell PDE activity, and modulating cytoskeletal organization. RX-RA 85 can be used in studies of rat breast cancer and metastatic tumors[1][2][3].
IC50 & Target
[3]|
PDE 2 nM (EC50) |
In Vitro
RX-RA 85 (2-16 μg/mL; 3 h) induces dose-dependent, partially reversible morphological changes in confluent bovine aortic endothelial cell monolayers, ranging from vacuolation at 2 μg/mL to complete cell rounding at 8-16 μg/mL[2].
RX-RA 85 (8 μg/mL; 8-96 h) causes significant differences in the sensitivity of endothelial cells derived from different species and organs, with bovine aortic endothelial cells showing the highest sensitivity and human meningeal endothelial cells the lowest[2].
RX-RA 85 (2-16 μg/mL; 60 min) induces dose-dependent cytotoxicity in B16-F1 melanoma cells, with high concentrations (8 μg/mL and 16 μg/mL) causing significant loss of membrane integrity and cell viability[2].
RX-RA 85 (4 μg/mL; 30 min) significantly alters the cytoskeletal organization of adherent B16-F1 cells located on the subendothelial matrix, disrupts microfilament-associated lamellipodial ruffling, and enhances the formation of microtubule complexes[2].
RX-RA 85 exhibits potent inhibitory activity against platelet phosphodiesterase, with an EC50 of 2 nM[3].
RX-RA 85 (8 μg/mL; 8-96 h) causes significant differences in the sensitivity of endothelial cells derived from different species and organs, with bovine aortic endothelial cells showing the highest sensitivity and human meningeal endothelial cells the lowest[2].
RX-RA 85 (2-16 μg/mL; 60 min) induces dose-dependent cytotoxicity in B16-F1 melanoma cells, with high concentrations (8 μg/mL and 16 μg/mL) causing significant loss of membrane integrity and cell viability[2].
RX-RA 85 (4 μg/mL; 30 min) significantly alters the cytoskeletal organization of adherent B16-F1 cells located on the subendothelial matrix, disrupts microfilament-associated lamellipodial ruffling, and enhances the formation of microtubule complexes[2].
RX-RA 85 exhibits potent inhibitory activity against platelet phosphodiesterase, with an EC50 of 2 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay[2]
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Cell Line:B16-F1 murine melanoma cells
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Concentration:2, 4, 8, 16 μg/mL
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Incubation Time:60 min
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Result:Results in 51Cr release of 6% at 2 μg/mL, 7% at 4 μg/mL, 16% at 8 μg/mL, and 23% at 16 μg/mL.
Results in 6% non-viable cells at 2 μg/mL, 15% non-viable cells at 4 μg/mL, 60% non-viable cells at 8 μg/mL, and 91% non-viable cells at 16 μg/mL.
In Vivo
RX-RA 85 (20 mg/kg/day; administered in drinking water; starting from day +1) significantly increases spleen weight and the number of IgM plaque-forming cells in the spleen of SRBC-immunized BALB/c mice on days 4 and 5 after immunization[3].
RX-RA 85 (20 mg/kg/day; administered in drinking water; 3 days) increases spleen weight in non-immunized BALB/c mice without altering the number of spontaneous splenic IgM PFC[3].
RX-RA 85 (20 mg/kg/day; dissolved in drinking water; administered starting from day -2, 0, +1, or +2 relative to SRBC immunization) enhances the primary immune response to SRBC by 2-fold, whereas administration 2 days prior to SRBC immunization produces only a moderate enhancing effect[3].
RX-RA 85 (2.5-40 mg/kg/day; administered in drinking water; starting from day +1) dose-dependently enhances the primary SRBC immune response, with IgM PFC counts reaching a plateau at 10 mg/kg/day and higher doses[3].
RX-RA 85 (10 mg/kg/day; administered in drinking water; relative to SRBC immunization, starting on day -2, day 0, day +1, or day +2) most potently enhances the primary SRBC immune response, with the most significant effects observed when administration begins on day +1 or day +2 after antigen immunization, whereas no significant immunoenhancement is seen when treatment starts 2 days before SRBC challenge[3].
RX-RA 85 (20 mg/kg/day; administered in drinking water; 3 days) increases spleen weight in non-immunized BALB/c mice without altering the number of spontaneous splenic IgM PFC[3].
RX-RA 85 (20 mg/kg/day; dissolved in drinking water; administered starting from day -2, 0, +1, or +2 relative to SRBC immunization) enhances the primary immune response to SRBC by 2-fold, whereas administration 2 days prior to SRBC immunization produces only a moderate enhancing effect[3].
RX-RA 85 (2.5-40 mg/kg/day; administered in drinking water; starting from day +1) dose-dependently enhances the primary SRBC immune response, with IgM PFC counts reaching a plateau at 10 mg/kg/day and higher doses[3].
RX-RA 85 (10 mg/kg/day; administered in drinking water; relative to SRBC immunization, starting on day -2, day 0, day +1, or day +2) most potently enhances the primary SRBC immune response, with the most significant effects observed when administration begins on day +1 or day +2 after antigen immunization, whereas no significant immunoenhancement is seen when treatment starts 2 days before SRBC challenge[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c male mice, 11-14 weeks old[3]
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Dosage:20 mg/kg/day
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Administration:in drinking water; starting from day +1
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Result:Reached a mean spleen weight of 237 mg at 4 days post-SRBC immunization.
Reached a mean PFC count of 498000 per spleen at 4 days post-SRBC immunization.\nReached a mean spleen weight of 216 mg at 5 days post-SRBC immunization.
Reached a mean PFC count of 253000 per spleen at 5 days post-SRBC immunization.
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Animal Model:BALB/c male mice, 11-14 weeks old[3]
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Dosage:20 mg/kg/day
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Administration:in drinking water; for 3 days
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Result:Reached a mean spleen weight of 179 mg in non-immunized mice.
Produced a mean of 233 spontaneous PFC per spleen with no change in spontaneous PFC numbers.
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Animal Model:BALB/c male mice, 11-14 weeks old[3]
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Dosage:20 mg/kg/day
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Administration:in drinking water; starting on day -2, 0, +1, or +2 relative to SRBC immunization
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Result:Produced a mean spleen weight of 193 mg and mean PFC count of 378000 per spleen when administration started on day -2.
Produced a mean spleen weight of 246 mg and mean PFC count of 563000 per spleen when administration started on day 0.
Produced a mean spleen weight of 212 mg and mean PFC count of 565000 per spleen when administration started on day +1.
Produced a mean spleen weight of 215 mg and mean PFC count of 581000 per spleen when administration started on day +2, representing an approximately 2-fold increase in the immune response relative to control animals.
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Animal Model:BALB/c male mice, 11-14 weeks old[3]
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Dosage:2.5, 5, 10, 20, 40 mg/kg/day
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Administration:in drinking water; starting from day +1
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Result:Reached a mean spleen weight of 155 mg and mean PFC count of 293000 per spleen at 2.5 mg/kg/day.
Reached a mean spleen weight of 180 mg and mean PFC count of 360000 per spleen at 5 mg/kg/day.
Reached a mean spleen weight of 204 mg and mean PFC count of 466000 per spleen at 10 mg/kg/day.
Reached a mean spleen weight of 207 mg and mean PFC count of 466000 per spleen at 20 mg/kg/day.
Reached a mean spleen weight of 238 mg and mean PFC count of 500000 per spleen at 40 mg/kg/day.
Showed a dose-dependent increase in immune response with a plateau in PFC counts reached at doses of 10 mg/kg/day or higher.
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Animal Model:BALB/c male mice, 11-14 weeks old[3]
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Dosage:10 mg/kg/day
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Administration:in drinking water; starting on day -2, 0, +1, or +2 relative to SRBC immunization
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Result:Produced a mean spleen weight of 179 mg and mean PFC count of 297000 per spleen when administration started on day -2.
Produced a mean spleen weight of 186 mg and mean PFC count of 341000 per spleen when administration started on day 0.
Produced a mean spleen weight of 191 mg and mean PFC count of 448000 per spleen when administration started on day +1.
Produced a mean spleen weight of 165 mg and mean PFC count of 406000 per spleen when administration started on day +2.
Exhibited the strongest stimulation of the immune response when administration was initiated after antigen administration on day +1 or +2, with no enhancement of PFC numbers when dosing started pre-immunization on day -2.
Related Protocols :
Chemical Information
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CAS No. 77749-81-6
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Masse moléculaire 469.63
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Formule C22H27N7OS2
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SMILES
O=S1CCN(C2=NC(=NC=3C(=NC=NC32)SCCC=4C=CC=CC4)N5CCNCC5)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
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RX-RA 85 Related Classifications
HY-187757 Related Classifications
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