289726-02-9 Usage
Uses
MPP is a high affinity silent antagonist at ERα.
Biological Activity
Selective, high affinity silent antagonist at ERa receptors. Displays > 200-fold selectivity for ERa over ERb. K i values are 2.7 and 1800 nM at ERa and ERb receptors respectively.
in vitro
mpp elicited significant apoptosis in the endometrial cancer cell lines, rl-95 cells, and ovine luminal endometrial cell lines relative to the vehicle-treated cells. it was indicated that selective estrogen receptor modulators-induced apoptosis is ascribed to genomic actions instead of toxicity, which was due to the low percentage of apoptosis reduced by the addition of a 10-fold excess of β-estradiol [1].
in vivo
wild-type (wt) cf1 and estrogen receptor-β knockout (erbko) female mice were injected intraperitoneally with two dosages 24 hr apart of 100 mg and 150 mg of mpp, 50 mg and 50 mg mpp, respectively. mpp significantly increased uterine weight and cell proliferation when compared to the vehicle control in wt and erbko mice. however, compared to the control groups, mpp did not effectively increase uterine wet weight. mpp treatment of ovariectomized mice activated apoptosis of the underlying uterine stromal cells without triggering apoptosis of the luminal epithelial cells [1].
IC 50
80 nm: blocks the transcriptional activation of the estrogen receptor (er) α.
references
[1]. davis, a., ellersieck, m., grimm, k., & rosenfeld, c. the effects of the selective estrogen receptor modulators, methyl-piperidino-pyrazole (mpp), and raloxifene in normal and cancerous endometrial cell lines and in the murine uterus. molecular reproduction and development. 2006; 73(8): 1034-1044.
Check Digit Verification of cas no
The CAS Registry Mumber 289726-02-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,8,9,7,2 and 6 respectively; the second part has 2 digits, 0 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 289726-02:
(8*2)+(7*8)+(6*9)+(5*7)+(4*2)+(3*6)+(2*0)+(1*2)=189
189 % 10 = 9
So 289726-02-9 is a valid CAS Registry Number.
289726-02-9Relevant academic research and scientific papers
Huang,Katzenellenbogen
, p. 2833 - 2836 (2000)
[reaction: see structure] A regioselective synthesis of 4-alkyl-1,3,5-triarylpyrazoles has been developed for the preparation of unsymmetrically substituted systems of interest as ligands for the estrogen receptor.
