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SQ22536

Cat. No. M6093
SQ22536 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 50  USD50 In stock
5mg USD 50  USD50 In stock
10mg USD 80  USD80 In stock
25mg USD 175  USD175 In stock
50mg USD 300  USD300 In stock
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Quality Control & Documentation
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.

Product Citations
Protocol (for reference only)
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.
Chemical Information
Molecular Weight 205.22
Formula C9H11N5O
CAS Number 17318-31-9
Solubility (25°C) DMSO 80 mg/mL
Water 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Olesen ET, et al. Am J Physiol Renal Physiol. The vasopressin type 2 receptor and prostaglandin receptors EP2 and EP4 can increase aquaporin-2 plasma membrane targeting through a cAMP-independent pathway.

[2] Liu K, et al. Neuropharmacology. The role of adenylyl cyclase in the medial prefrontal cortex in cocaine-induced behavioral sensitization in rats.

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