A TRPP3 inhibitor (IC50 = 140 nM); also inhibits ENaC (IC50 = 400 nM); decreases basal short-circuit currents in human and ovine bronchial epithelial cells (IC50s = 75 and 116 nM

Phenamil (methanesulfonate) – 10 mg

Brand:
Cayman
CAS:
1161-94-0
Storage:
-20
UN-No:
Non-Hazardous - /

Phenamil is an inhibitor of transient receptor potential polycystin-L (TRPP3; IC50 = 140 nM) and a derivative of amiloride (Item No. 14409).{24798} It also inhibits the epithelial sodium channel (ENaC; IC50 = 400 nM).{55255} Phenamil decreases basal short-circuit currents in human and ovine bronchial epithelial cells with IC50 values of 75 and 116 nM, respectively.{24797} It inhibits potassium chloride-induced contractions in isolated rat endothelium-denuded aortic rings (EC50 = 6.76 µM) and increases contractile force in isolated rat right ventricular papillary muscles (EC50 = 16.98 µM).{55253} Phenamil (15 and 30 mg/kg per day) reduces pulmonary artery medial wall thickness and decreases right ventricular peak pressure in a rat model of chronic hypoxia-induced pulmonary hypertension.{55254}  

 

Add to quotes
SKU: - Category:

Description

A TRPP3 inhibitor (IC50 = 140 nM); also inhibits ENaC (IC50 = 400 nM); decreases basal short-circuit currents in human and ovine bronchial epithelial cells (IC50s = 75 and 116 nM, respectively); inhibits potassium chloride-induced contractions in isolated rat endothelium-denuded aortic rings (EC50 = 6.76 µM) and increases contractile force in isolated rat right ventricular papillary muscles (EC50 = 16.98 µM); reduces pulmonary artery medial wall thickness and decreases right ventricular peak pressure in a rat model of chronic hypoxia-induced pulmonary hypertension at 15 and 30 mg/kg per day

Formal name: 3,5-diamino-6-chloro-N-[imino(phenylamino)methyl]-2-pyrazinecarboxamide, monomethanesulfonate

Synonyms: 

Molecular weight: 401.8

CAS: 1161-94-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Immunology & Inflammation|Pulmonary Diseases

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
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 5 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 5 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
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 1 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 - 1 mg

    Available on backorder

    Add to quotes
    View product page