In vitro: SQ22536(250 µmol/L) attenuates the inhibitory effect of adenosine against ADP-induced platelet aggregation from 8±5 to 57±5%, respectively (p<0.001). SQ22536 also attenuates an increase of intraplatelet levels of cAMP by adenosine from 29±2 to 9±1 pmol/108 platelets (p<0.05). It has no effect on the platelet antiaggregant activity of inosine (1 to 4 mmol/L) and ADP-induced platelet aggregation. In vivo: SQ22536 abolishes the renal protective effects of liraglutide in KK/Ta-Akita mice. the amelioration of glomerular histopathological damage by liraglutide is eliminated in KK/Ta-Akita mice treated with liraglutide in combination with SQ22536. Renal cAMP does not increase after treatment with SQ22536. In a word, the beneficial actions of liraglutide for treatment of nephropathy are inhibited by the adenylate cyclase inhibitor SQ22536.
Cell Experiment | |
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Cell lines | Human leukemic mast cell line(HMC-1) and human umbilical cord blood-derived mast cell(hCBMCs) |
Preparation method | HMC-1 cells and hCBMCs are plated in 48-well plates and serum-starved overnight. The next day, cells are preincubated with SQ22536 at the indicated concentrations for 30 min before stimulation with CRH (100 nM for HMC-1 or 1 μM for hCBMC) for 3 min in the presence or absence of SQ22536 in serum-free culture media. Cell lysates are then prepared and assayed for protein kinase A activity using ELISA. |
Concentrations | 0.1, 1, 10 mM |
Incubation time | 30 min |
Animal Experiment | |
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Animal models | Male C57BL/6J mice |
Formulation | Saline |
Dosages | 10 mg/kg |
Administration | s.c. |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Molecular Weight | 205.22 |
Formula | C9H11N5O |
CAS Number | 17318-31-9 |
Purity | >98% |
Solubility | 41 mg/mL in DMSO |
Storage | at -20°C |
The vasopressin type 2 receptor and prostaglandin receptors EP2 and EP4 can increase aquaporin-2 plasma membrane targeting through a cAMP-independent pathway.
Olesen ET, et al. Am J Physiol Renal Physiol. 2016 Nov 1;311(5):F935-F944. PMID: 27558562.
The role of adenylyl cyclase in the medial prefrontal cortex in cocaine-induced behavioral sensitization in rats.
Liu K, et al. Neuropharmacology. 2016 Dec;111:70-77. PMID: 27020043.
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