A μ-opioid receptor antagonist (Ki = 0.47 nM); selective over κ- and δ-opioid receptors (Kis= 100 nM and 12 nM

Alvimopan – 25 mg

Brand:
Cayman
CAS:
156053-89-3
Storage:
-20
UN-No:
Non-Hazardous - /

Alvimopan is a peripherally acting μ-opioid receptor antagonist (Ki = 0.47 nM) that is selective over the κ- and δ-opioid receptors (Kis= 100 nM and 12 nM, respectively).{25494} In vitro, alvimopan inhibits μ-opioid receptor-mediated GTP binding to CHO cell membranes with an IC50 value of 1.7 nM. Alvimopan reduces morphine-induced inhibition of gastrointestinal (GI) transit in rats, guinea pigs, and mice more potently than methylnaltrexone (Item No. 24072) or naloxone (Item No. 15594).{39510} It inhibits morphine-induced slowing of colorectal transit in mice with an ED50 value of 0.41 mg/kg. Orally administered alvimopan (0.3 and 1 mg/kg, p.o.) reduces the inhibition of GI transit induced by morphine (Item No. ISO60147) but not by apraclonidine (Item No. 23904) in rats, suggesting that alvimopan does not act in the CNS. Formulations containing alvimopan have been used to treat opioid-induced bowel dysfunction.  

 

Available on backorder

Add to quotes
SKU: 23902 - 25 mg Category:

Description

A μ-opioid receptor antagonist (Ki = 0.47 nM); selective over κ- and δ-opioid receptors (Kis= 100 nM and 12 nM, respectively); inhibits μ-opioid receptor mediated GTP binding to CHO cell membranes (IC50 = 1.7 nM); inhibits morphine-induced slowing of colorectal transit in mice (ED50 = 0.41 mg/kg, p.o.); antagonizes morphine-but not apraclonidine-induced inhibition of GI transit in rats (0.3 and 1 mg/kg, p.o.)

Formal name: N-[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]-glycine

Synonyms:  ADL 8-2698|LY246736

Molecular weight: 424.5

CAS: 156053-89-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

Related products

  • 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
    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 – 500 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 - 500 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
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 250 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 - 250 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page