A 5-HT2C receptor antagonist; binds to 5-HT2C receptors (Ki = 3.8 nM for the recombinant human receptor) and is selective for 5-HT2C receptors over 5-HT2A and 5-HT2B receptors (Kis = 1

RS 102221 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
187397-18-8
Storage:
-20
UN-No:
Non-Hazardous - /

RS 102221 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2C.{53989} It binds to 5-HT2C receptors (Ki = 3.8 nM for the recombinant human receptor) and is selective for 5-HT2C receptors over 5-HT2A and 5-HT2B receptors (Kis = 1,122.02 and 812.83 nM, respectively), as well as a panel of additional neurotransmitter receptors and ion channels (Kis = ≥316.23 nM for all). RS 102221 inhibits 5-HT-induced increases in the extracellular media acidification rate of CHO-K1 cells expressing human 5-HT2C receptors (pA2 = 8.1). It increases food intake and weight gain in rats when administered at a dose of 2 mg/kg. RS 102221 (2 mg/kg) increases the time spent in the light compartment in the light-dark exploration test in mice and reduces prepulse inhibition of the startle reflex when administered at a dose of 1 mg/kg.{53990}  

 

Available on backorder

Add to quotes
SKU: 31543 - 1 mg Category:

Description

A 5-HT2C receptor antagonist; binds to 5-HT2C receptors (Ki = 3.8 nM for the recombinant human receptor) and is selective for 5-HT2C receptors over 5-HT2A and 5-HT2B receptors (Kis = 1,122.02 and 812.83 nM, respectively), as well as a panel of additional neurotransmitter receptors and ion channels (Kis = ≥316.23 nM for all); inhibits 5-HT-induced increases in the extracellular media acidification rate of CHO-K1 cells expressing human 5-HT2C receptors (pA2 = 8.1); increases food intake and weight gain in rats at 2 mg/kg; increases the time spent in the light compartment in the light-dark exploration test in mice at 2 mg/kg; reduces prepulse inhibition of the startle reflex in mice at 1 mg/kg

Formal name: N-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)-benzenesulfonamide, monohydrochloride

Synonyms: 

Molecular weight: 649.1

CAS: 187397-18-8

Purity: ≥98%

Formulation: A solid

Related products

  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 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 – 25 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 - 25 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 – 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
    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 – 500 µg

    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 - 500 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page