SQ22536

Synonyms: 9-(tetrahydrofuran-2-yl)-9h-purin-6-amine

SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine) is an inhibitor of adenylyl cyclase with an IC50 of 1.4 μM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.

SQ22536 Chemical Structure

SQ22536 Chemical Structure

CAS No. 17318-31-9

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Signaling Pathway

Biological Activity

Description SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine) is an inhibitor of adenylyl cyclase with an IC50 of 1.4 μM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.
Targets
Adenylyl cyclase [1]
In vitro
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[4].

Cell Research Cell lines Human leukemic mast cell line(HMC-1) and human umbilical cord blood-derived mast cell(hCBMCs)
Concentrations 0.1, 1, 10 mM
Incubation Time 30 min
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.

In Vivo
In vivo

SQ22536 abolishes the renal protective effects in KK/Ta-Akita mice. the amelioration of glomerular histopathological damage is eliminated in KK/Ta-Akita mice treated with SQ22536. Renal cAMP does not increase after treatment with SQ22536. In a word, the beneficial actions for treatment of nephropathy are inhibited by the adenylate cyclase inhibitor SQ22536[5].

Animal Research Animal Models Male C57BL/6J mice
Dosages 10 mg/kg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 205.22 Formula

C9H11N5O

CAS No. 17318-31-9 SDF Download SQ22536 SDF
Smiles C1CC(OC1)N2C=NC3=C(N=CN=C32)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 41 mg/mL ( (199.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 41 mg/mL

Ethanol : 41 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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