An active metabolite of tolterodine and fesoterodine; inhibits M1-5 muscarinic receptors (Kis = 2.3

5-hydroxymethyl Tolterodine (formate) – 1 mg

Brand:
Cayman
CAS:
380636-49-7
Storage:
-20
UN-No:
Non-Hazardous - /

5-hydroxymethyl Tolterodine is an active metabolite of the muscarinic acetylcholine receptor antagonists tolterodine (Item No. 15027) and fesoterodine (Item No. 23777).{47319} It is formed from tolterodine by the cytochrome P450 (CYP) isoform CYP2D6 and from fesoterodine by plasma esterases.{47320,47319} 5-hydroxymethyl Tolterodine inhibits M1-5 muscarinic receptors with Ki values of 2.3, 2, 2.5, 2.8, and 2.9 nM, respectively, for the human receptors expressed in CHO cells.{47321} It selectively inhibits acetylcholine-induced bladder contraction over electrically induced salivation in anesthetized cats (ID50s = 15 and 40 nmol/kg, respectively).  

 

Available on backorder

Add to quotes
SKU: 27833 - 1 mg Category:

Description

An active metabolite of tolterodine and fesoterodine; inhibits M1-5 muscarinic receptors (Kis = 2.3, 2, 2.5, 2.8, and 2.9 nM, respectively); selectively inhibits acetylcholine-induced bladder contraction over electrically induced salivation in anesthetized cats (ID50s = 15 and 40 nmol/kg, respectively)

Formal name: formic acid, compd. with 3-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxybenzenemethanol

Synonyms:  5-HMT|Desfesoterodine|PNU 200577

Molecular weight: 387.5

CAS: 380636-49-7

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

Related products

  • 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
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 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 - 10 µg

    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) – 500 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 - 500 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page