An antagonist of muscarinic acetylcholine receptors (Kis = 5

Oxybutynin (hydrochloride) – 10 g

Brand:
Cayman
CAS:
1508-65-2
Storage:
-20
UN-No:
Non-Hazardous - /

Oxybutynin is an antagonist of muscarinic acetylcholine receptors (Kis = 5, 14.5, 3.7, 5.3, and 40 nM for human recombinant M1-5, respectively).{39586} It inhibits intracellular calcium mobilization induced by carbamoylcholine (carbachol; Item No. 14486) in bladder smooth muscle and submandibular gland cells isolated from cynomolgus monkeys (Kis = 2 and 1 nM, respectively).{39587} Oxybutynin inhibits volume-induced bladder contraction (VIBC) and oxotremorine-induced salivation (OIS) in rats (ID50s = 0.062 and 0.089 mg/kg, respectively).{39586} It also increases pupil diameter (PD) and locomotor activity (LMA; ED50s = 0.29 and 0.52 mg/kg, respectively) and decreases small intestinal transit (SIT; ID50 = 0.22 mg/kg) in rats. Formulations containing oxybutynin have been used in the treatment of overactive bladder.  

 

Available on backorder

Add to quotes
SKU: 23825 - 10 g Category:

Description

An antagonist of muscarinic acetylcholine receptors (Kis = 5, 14.5, 3.7, 5.3, and 40 nM for human recombinant M1-5, respectively); inhibits carbachol- induced intracellular calcium mobilization in bladder smooth muscle and submandibular gland cells isolated from cynomolgus monkeys (Kis = 2 and 1 nM, respectively); inhibits VIBC and OIS in rats (ID50s = 0.062 and 0.089 mg/kg, respectively); increases PD and LMA (ED50s = 0.29 and 0.52 mg/kg, respectively) and decreases SIT (ID50 = 0.22 mg/kg) in rats

Formal name: 4-(diethylamino)-2-butyn-1-yl ester α-cyclohexyl-α-hydroxy-benzeneacetic acid, monohydrochloride

Synonyms:  MJ4309-1

Molecular weight: 394

CAS: 1508-65-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Ophthalmology

Related products

  • 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
  • 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
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 10 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 - 10 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