Abcam, ab141273, Cilostamide, PDE3 inhibitor

Size: 10mg / 50mg
MW 342.4 Da, Purity >98%. Potent, selective PDE3 inhibitor (IC 50 values are 27 and 50 nM for PDE3A and PDE3B, respectively). Inhibits ADP-induced platelet aggregation (IC 50 = 16.8 μM). Antithrombotic effects in vivo. Orally active.
Key facts
CAS number:68550-75-4,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:342.4 Da,
Molecular formula:C20H26N2O3,
PubChem:2753,
Nature:Synthetic,
Solubility:Soluble in DMSO to 100 mM,
Biochemical name:Cilostamide,
Biological description:Potent, selective PDE3 inhibitor (IC50 values are 27 and 50 nM for PDE3A and PDE3B, respectively). Inhibits ADP-induced platelet aggregation (IC50 = 16.8 μM). Antithrombotic effects in vivo. Orally active.,
Canonical smiles:CN(C1CCCCC1)C(=O)CCCOC2=CC3=C(C=C2)NC(=O)C=C3,
InChi:InChI=1S/C20H26N2O3/c1-22(16-6-3-2-4-7-16)20(24)8-5-13-25-17-10-11-18-15(14-17)9-12-19(23)21-18/h9-12,14,16H,2-8,13H2,1H3,(H,21,23),
InChiKey:UIAYVIIHMORPSJ-UHFFFAOYSA-N,
IUPAC Name:N-cyclohexyl-N-methyl-4-[(2-oxo-1H-quinolin-6-yl)oxy]butanamide

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions-Ambient, Storage information-The product can be stored for up to 12 months

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
The Estrogen Receptor (ER) and TSH Receptor (TSH-R) are proteins involved in hormone signaling. Estrogen Receptor about 66 kDa is expressed in tissues like breast uterus and ovaries responding to estrogen hormone. TSH Receptor or thyrotropin receptor found in the thyroid gland is critical for thyroid function. Proteins like Gli3 are transcriptional regulators involved in development. Pregnane X Receptor (PXR) is a nuclear receptor that controls expression of genes in liver and intestine. Phosphodiesterase (PDE) family enzymes including PDE1A PDE1B PDE1C PDE3A PDE3B and PDE5A play roles in cyclic nucleotide breakdown affecting cellular signaling. PAF-R or platelet-activating factor receptor is a G-coupled receptor involved in immune responses.
Biological function summary
Estrogen Receptor helps regulate gene expression influencing cell proliferation and differentiation often interacting with co-regulators like SRC-1. TSH Receptor enables thyroid hormone production affecting metabolism. Gli3 functions in limb and brain development part of Shh signaling complex. PXR modulates xenobiotic metabolism engaging with CYP3A4 enzyme. PDE enzymes degrade cAMP and cGMP influencing muscle contraction learning and memory. PDE inhibitors have pharmaceutical applications targeting these processes. PAF-R activation leads to inflammation by engaging downstream signaling pathways.
Pathways
Estrogen Receptor is integral to estrogen signaling and interacts with proteins like HER2 impacting cellular growth pathways. TSH Receptor participates in thyroid hormone synthesis through the cAMP signaling pathway. Gli3 relates to Sonic Hedgehog (Shh) pathway coordinating with proteins such as SUFU. PXR links with xenobiotic metabolism pathways involving enzymes like CYP450. PDEs are in cyclic nucleotide metabolism impacting vasodilation pathways along with proteins like nitric oxide synthase.
Estrogen Receptor involvement is significant in breast cancer where it correlates with HER2. Abnormal TSH Receptor function can cause Graves’ disease an autoimmune disorder affecting the thyroid also linked to autoantibodies against thyroglobulin. Gli3 mutations associate with polydactyly and holoprosencephaly. PXR polymorphisms might influence drug metabolism affecting treatment efficacy. PDE dysfunction impacts cardiovascular diseases and erectile dysfunction where PDE5 inhibitors are therapeutic. PAF-R overactivity connects to asthma and inflammation disorders mediated by cytokines.