A non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase

Fadrozole (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
102676-31-3
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).{38819,38820} It selectively inhibits estrogen over progesterone production induced by luteinizing hormone (LH) in hamster ovarian tissue as well as corticosterone and aldosterone production induced by adrenocorticotropic hormone (ACTH; Item No. 24257) in rat adrenal tissue (IC50s = 0.03, 160, 100, and 1 μM, respectively).{38819} It also decreases ovarian estrogen levels in rats when administered at a dose of 0.26 mg/kg.{38820} Fadrozole inhibits conversion of cholesterol to 27-hydroxycholesterol by the cytochrome P450 (CYP) isomer 27A1 (Ki = 4.6 μM).{38821} It inhibits growth of androstenedione-stimulated mammary D2 cells implanted into thoracic mammary fat pads of mice by 95% when administered at a dose of 0.5 mg per animal per day.{38822}  

 

Available on backorder

Add to quotes
SKU: 24272 - 10 mg Category:

Description

A non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively); selectively inhibits LH-induced estrogen over progesterone production in hamster ovarian tissue as well as ACTH-induced corticosterone and aldosterone production in rat adrenal tissue (IC50s = 0.03, 160, 100, and 1 μM, respectively); decreases ovarian estrogen levels in rats (0.26 mg/kg); inhibits growth of androstenedione-stimulated mammary D2 cells implanted in mice by 95% (0.5 mg per animal per day) ,

Formal name: 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, monohydrochloride

Synonyms:  CGS 16949A

Molecular weight: 259.7

CAS: 102676-31-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Glucocorticoids & Mineralocorticoids

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 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 - 100 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 – 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
  • 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; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 10 mg

    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.  

     

    Brand:
    Cayman
    SKU:10009557 - 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 – 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