An anthranilic acid derivative that activates the oxidized (heme-free) form of sGC (EC50 = 0.5-10 µM in purified bovine lung or crude human corpus cavernosum) by binding to the heme pocket and mimicking its function; increases cGMP levels in cultured rat aorta smooth muscle cells and induces vasorelaxation of isolated rat aorta

Ataciguat – 10 mg

Brand:
Cayman
CAS:
254877-67-3
Storage:
-20
UN-No:
Non-Hazardous - /

Soluble guanylate cyclase (sGC) is the primary cellular receptor for NO. NO binds and activates a heme group in sGC, initiating the conversion of GTP to the second messenger cGMP. cGMP subsequently mediates a number of signaling cascades leading to vasorelaxation and inhibiting smooth muscle proliferation, leukocyte recruitment, and platelet aggregation. Oxidation of the heme results in its dissociation from sGC and an impairment of NO signaling, which has been linked to hypertension, hyperlidemia, cardiovascular disease, and diabetes.{26751} Ataciguat is an anthranilic acid derivative that activates the oxidized (heme-free) form of sGC (EC50 = 0.5-10 µM in purified bovine lung or crude human corpus cavernosum isolates) by binding to the heme pocket and mimicking its function.{26751,26750,26752} It has been shown to increase cGMP levels in cultured rat aorta smooth muscle cells and to induce vasorelaxation of isolated rat aorta, porcine coronary arteries, and human corpus cavernosum (EC50 = 1-10 µM).{26750}  

 

Out of stock

Add to quotes
SKU: - Category:

Description

An anthranilic acid derivative that activates the oxidized (heme-free) form of sGC (EC50 = 0.5-10 µM in purified bovine lung or crude human corpus cavernosum) by binding to the heme pocket and mimicking its function; increases cGMP levels in cultured rat aorta smooth muscle cells and induces vasorelaxation of isolated rat aorta, porcine coronary arteries, and human corpus cavernosum isolates (EC50 = 1-10 µM)

Formal name: 5-chloro-2-[[(5-chloro-2-thienyl)sulfonyl]amino]-N-[4-(4-morpholinylsulfonyl)phenyl]-benzamide

Synonyms:  HMR 1766

Molecular weight: 576.5

CAS: 254877-67-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators|Cyclases||Research Area|Cardiovascular System|Vasculature|Vasodilation

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 250 mg

    Available on backorder

    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 25 µg

    Available on backorder

    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 10 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 10 mg

    Available on backorder

    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

    Add to quotes
    View product page