SQ22536

Catalog No.S8283 Batch:S828301

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Technical Data

Formula

C9H11N5O
Molecular Weight 205.22 CAS No. 17318-31-9
Solubility (25°C)* In vitro DMSO 41 mg/mL (199.78 mM)
Water 41 mg/mL (199.78 mM)
Ethanol 41 mg/mL (199.78 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].
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[5].

Protocol (from reference)

Cell Assay:[2]
  • 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.
Animal Study:[3]
  • Animal Models

    Male C57BL/6J mice

  • Dosages

    10 mg/kg

  • Administration

    s.c.

Customer Product Validation

Data from [Data independently produced by , , ONCOLOGY REPORTS, 2017, 37:3572-3580]

Data from [Data independently produced by , , J Food Sci, 2018, 83(9):2394-2401]

Selleck's SQ22536 has been cited by 22 publications

Promoting collateral formation in type 2 diabetes mellitus using ultra-small nanodots with autophagy activation and ROS scavenging [ J Nanobiotechnology, 2024, 22(1):85] PubMed: 38429826
Suppression of cAMP/PKA/CREB signaling ameliorates retinal injury in diabetic retinopathy [ Kaohsiung J Med Sci, 2023, 10.1002/kjm2.12722] PubMed: 37338034
ACE2 pathway regulates thermogenesis and energy metabolism [ Elife, 2022, 11e72266] PubMed: 35014608
Regulation of CRE-Dependent Transcriptional Activity in a Mouse Suprachiasmatic Nucleus Cell Line [ Int J Mol Sci, 2022, 23-2012226] PubMed: 36293078
Atorvastatin inhibits neuronal apoptosis via activating cAMP/PKA/p-CREB/BDNF pathway in hypoxic-ischemic neonatal rats [ FASEB J, 2022, 36(4):e22263] PubMed: 35303316
Targeting adipocytic discoidin domain receptor 2 impedes fat gain while increasing bone mass [ Cell Death Differ, 2021, 10.1038/s41418-021-00887-9] PubMed: 34645939
FOSL2 promotes VEGF-independent angiogenesis by transcriptionnally activating Wnt5a in breast cancer-associated fibroblasts [ Theranostics, 2021, 11(10):4975-4991] PubMed: 33754039
Conjugated secondary 12α-hydroxylated bile acids promote liver fibrogenesis [ EBioMedicine, 2021, 66:103290] PubMed: 33752128
Microglial MT1 activation inhibits LPS-induced neuroinflammation via regulation of metabolic reprogramming [ Aging Cell, 2021, e13375] PubMed: 33964119
ER stress-induced adipocytes secrete-aldo-keto reductase 1B7-containing exosomes that cause nonalcoholic steatohepatitis in mice [ Free Radic Biol Med, 2021, 163:220-233] PubMed: 33359683

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.