Product Name :
Methylpiperidino pyrazole
Description:
IC50: 80 nM: blocks the transcriptional activation of the estrogen receptor (ER) α. Methylpiperidino pyrazole, also named as MPP, is an ER antagonist with highly selective for ERα compared to ERβ. MPP inhibits the transcriptional activation of ERα and has been used to assess the role of ERα in a wide range of estrogen-responsive systems which include certain cancers. Two ER subtypes, ERα and ERβ, are involved in the mediation of estrogen action, which exerts different effects on cellular processes including proliferation, apoptosis and migration, as well as opposite influence on the development and progression of cancer. 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 . 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 .
CAS:
289726-02-9
Molecular Weight:
469.57
Formula:
C29H31N3O3
Chemical Name:
4-[3-(4-hydroxyphenyl)-4-methyl-5-{4-[2-(piperidin-1-yl)ethoxy]phenyl}-1H-pyrazol-1-yl]phenol
Smiles :
CC1C(=NN(C=1C1C=CC(=CC=1)OCCN1CCCCC1)C1C=CC(O)=CC=1)C1C=CC(O)=CC=1
InChiKey:
TXLGPGWHIIHRHH-UHFFFAOYSA-N
InChi :
InChI=1S/C29H31N3O3/c1-21-28(22-5-11-25(33)12-6-22)30-32(24-9-13-26(34)14-10-24)29(21)23-7-15-27(16-8-23)35-20-19-31-17-3-2-4-18-31/h5-16,33-34H,2-4,17-20H2,1H3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
IC50: 80 nM: blocks the transcriptional activation of the estrogen receptor (ER) α. Methylpiperidino pyrazole, also named as MPP, is an ER antagonist with highly selective for ERα compared to ERβ. MPP inhibits the transcriptional activation of ERα and has been used to assess the role of ERα in a wide range of estrogen-responsive systems which include certain cancers. Two ER subtypes, ERα and ERβ, are involved in the mediation of estrogen action, which exerts different effects on cellular processes including proliferation, apoptosis and migration, as well as opposite influence on the development and progression of cancer. 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 . 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.{{Carmofur} web|{Carmofur} Metabolic Enzyme/Protease|{Carmofur} Activator|{Carmofur} Purity & Documentation|{Carmofur} In stock|{Carmofur} manufacturer} MPP significantly increased uterine weight and cell proliferation when compared to the vehicle control in WT and ERbKO mice.{{Ethacrynic acid} site|{Ethacrynic acid} Immunology/Inflammation|{Ethacrynic acid} Technical Information|{Ethacrynic acid} In Vitro|{Ethacrynic acid} supplier|{Ethacrynic acid} Autophagy} However, compared to the control groups, MPP did not effectively increase uterine wet weight.PMID:32472497 MPP treatment of ovariectomized mice activated apoptosis of the underlying uterine stromal cells without triggering apoptosis of the luminal epithelial cells .|Product information|CAS Number: 289726-02-9|Molecular Weight: 469.57|Formula: C29H31N3O3|Chemical Name: 4-[3-(4-hydroxyphenyl)-4-methyl-5-{4-[2-(piperidin-1-yl)ethoxy]phenyl}-1H-pyrazol-1-yl]phenol|Smiles: CC1C(=NN(C=1C1C=CC(=CC=1)OCCN1CCCCC1)C1C=CC(O)=CC=1)C1C=CC(O)=CC=1|InChiKey: TXLGPGWHIIHRHH-UHFFFAOYSA-N|InChi: InChI=1S/C29H31N3O3/c1-21-28(22-5-11-25(33)12-6-22)30-32(24-9-13-26(34)14-10-24)29(21)23-7-15-27(16-8-23)35-20-19-31-17-3-2-4-18-31/h5-16,33-34H,2-4,17-20H2,1H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|