Methylpiperidino pyrazole

CAS No. 289726-02-9

Methylpiperidino pyrazole( —— )

Catalog No. M27481 CAS No. 289726-02-9

Methylpiperidino pyrazole is an ERα inhibitor and can prevent the BPS-induced Rb phosphorylation and cell cycle progression.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 53 In Stock
5MG 77 In Stock
10MG 143 In Stock
25MG 314 In Stock
50MG 588 In Stock
100MG 881 In Stock
200MG 1322 In Stock
500MG Get Quote In Stock
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Biological Information

  • Product Name
    Methylpiperidino pyrazole
  • Note
    Research use only, not for human use.
  • Brief Description
    Methylpiperidino pyrazole is an ERα inhibitor and can prevent the BPS-induced Rb phosphorylation and cell cycle progression.
  • Description
    Methylpiperidino pyrazole is an ERα inhibitor and can prevent the BPS-induced Rb phosphorylation and cell cycle progression.
  • In Vitro
    MPP (1, 5, 10, 25, 50 and 100 μM; 24 h) decreases cell viability with an IC50 value of 20.01 μM in RL95-2 cells.MPP dihydrochloride shows antiproliferative activity at a concentration of 10 μM inRL95-2 cells.MPP dihydrochloride (20 μM; 24 h) reduces the phosphorylation of ERα, while it does not alter the phosphorylation of Akt. MPP dihydrochloride reduces the ratio of p-ERα/ERα.Cell Viability Assay Cell Line:RL95-2 endometrium cancer cells Concentration:1, 5, 10, 25, 50 and 100 μM Incubation Time:24 hours Result:The treatment with 25 μM, 50 μM and 100 μM for 24 h decreased cell viability significantly. However, cell viability was not significantly changed by MPP dihydrochloride at concentration below 25 μM.Cell Proliferation Assay Cell Line:RL95-2 cell Concentration:10, 15, 20 and 25 μM Incubation Time:72 hours Result:Showed antiproliferative activity at a concentration of 10 μM.Western Blot Analysis Cell Line:RL95-2 cell line Concentration:20 μM Incubation Time:24 hours Result:Reduced the phosphorylation of ERα, while it did not alter the phosphorylation of Akt. Reduced the ratio of p-ERα/ERα compared to the control group.
  • In Vivo
    MPP (Low dose 20 μg/kg body weight or high dose 200 μg/kg body weight) leads to a dose-dependent attenuation of percent prepulse inhibition (PPI). Animal Model:Male C57BL/6N mice at the age of 9-10 weeksDosage:Low dose (20 μg/kg body weight) or high dose (200 μg/kg body weight) Administration:Administered subcutaneously (s.c.) injected; injection volume of 5 mL/kg; 60 min before PPI testing Result:Led to a dose-dependent attenuation of percent PPI. Pretreatment with 200 μg/kg reduced the mean percent PPI scores by ~30%.
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    289726-02-9
  • Formula Weight
    469.57
  • Molecular Formula
    C29H31N3O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    Cc1c(-c(cc2)ccc2OCCN2CCCCC2)n(-c(cc2)ccc2O)nc1-c(cc1)ccc1O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Robinson DM, Keating GM. Colesevelam: a review of its use in hypercholesterolemia. Am J Cardiovasc Drugs. 2007;7(6):453-65.
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