An NK3 receptor antagonist (IC50 = 18.4 nM); selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100

SB 222200 – 25 mg

Brand:
Cayman
CAS:
174635-69-9
Storage:
-20
UN-No:
Non-Hazardous - /

SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}  

 

Available on backorder

Add to quotes
SKU: 29422 - 25 mg Category:

Description

An NK3 receptor antagonist (IC50 = 18.4 nM); selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively); decreases neurokinin B-induced calcium mobilization (IC50 = 265 nM in HEK293 cells expressing the recombinant human receptor); inhibits senktide-induced contractions in isolated rabbit iris sphincter muscle at 300 nM; decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats at 500 pmol, i.c.v.; prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg)

Formal name: 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide

Synonyms: 

Molecular weight: 380.5

CAS: 174635-69-9

Purity: ≥95%

Formulation: A crystalline solid

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
    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
    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 – 100 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 - 100 mg

    Available on backorder

    Add to quotes
    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 – 1 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 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page