Oxybutynin-d10 is intended for use as an internal standard for the quantification of oxybutynin (Item No. 23825) by GC- or LC-MS. 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.
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An internal standard for the quantification of oxybutynin by GC- or LC-MS
Formal name: benzeneacetic acid, α-cyclohexyl-α-hydroxy-4-[di(ethyl-d5)amino]-2-butynyl ester, monohydrochloride
Synonyms:
Molecular weight: 404
CAS: 120092-65-1
Purity: ≥99% deuterated forms (d1-d10)
Formulation: A solid
Application|Mass Spectrometry||Product Type|Biochemicals|Analytical Standards||Product Type|Biochemicals|Isotopically Labeled Standards|Deuterium||Research Area|Neuroscience|Ophthalmology
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.
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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}
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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.
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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}
Available on backorder