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SQ22536

Cat. No. M6093
SQ22536 Structure
Size Price Availability
10mg USD 95 4-7 Days
25mg USD 200 4-7 Days
50mg USD 370 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
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
Animal models Male C57BL/6J mice
Formulation Saline
Dosages 10 mg/kg
Administration s.c.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 205.22
Formula C9H11N5O
CAS Number 17318-31-9
Purity >98%
Solubility 41 mg/mL in DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SQ22536 supplier, Fluorescent Dye, inhibitors

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