304853-42-7 Usage
Uses
Oral contraception; nonsteroidal ligand for the progesterone receptor.
Biological Activity
tanaproget is a novel agonist of progesterone receptor with ic50 of 1.7 nm [1].progesterone receptor (pr) is a member of the nuclear receptor superfamily and binding of progesterone causes pr conformational changes, which then changing gene expression. progesterone plays an important role in female reproduction [1].in t47d cells, tanaproget caused alkaline phosphatase activity with ec50 value of 0.1 nm. in a mammalian two-hybrid assay, tanaproget showed 50-fold more potent than progesterone. in stromal cells isolated from endometrial, tanaproget (1 nm) significantly suppressed pro-mmp-3 secretion. also, tanaproget effectively prevented pro-mmp-3 secretion through il-1α-mediated stimulation [2].in endometriosis mice model with human lesions growing on the parietal peritoneum of mice, tanaproget completely regressed human lesions in 58% treated animals. also, the lesions were smaller and fewer compared with the lesions in placebo-treated mice at the end of therapy [2]. in healthy women, the elimination half-life (t(1/2)) of tanaproget ranged from 12 to 30 h. tanaproget reduced cervical mucus scores, which suggesting poor production and quality of cervical mucus [3].
references
[1]. zhang z, olland am, zhu y, et al. molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget. j biol chem, 2005, 280(31): 28468-28475. [2]. bruner-tran kl, zhang z, eisenberg e, et al. down-regulation of endometrial matrix metalloproteinase-3 and -7 expression in vitro and therapeutic regression of experimental endometriosis in vivo by a novel nonsteroidal progesterone receptor agonist, tanaproget. j clin endocrinol metab, 2006, 91(4): 1554-1560.[3]. bapst jl, ermer jc, ferron gm, et al. pharmacokinetics and safety of tanaproget, a nonsteroidal progesterone receptor agonist, in healthy women. contraception, 2006, 74(5): 414-418.
Check Digit Verification of cas no
The CAS Registry Mumber 304853-42-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,0,4,8,5 and 3 respectively; the second part has 2 digits, 4 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 304853-42:
(8*3)+(7*0)+(6*4)+(5*8)+(4*5)+(3*3)+(2*4)+(1*2)=127
127 % 10 = 7
So 304853-42-7 is a valid CAS Registry Number.
304853-42-7Relevant articles and documents
COMPOSITIONS CONTAINING TANAPROGET AND NATURAL ESTROGENS
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Paragraph 00027; 00090; 00097-00099, (2014/10/15)
The present invention provides compositions containing Tanaproget and a natural estrogen. In one embodiment, the natural estrogen is 17β-estradiol or E4. Also provided are drug delivery devices and kits containing these compounds and compositions and meth
Methods for minimizing thioamide impurities
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Page/Page column 7-8, (2008/06/13)
Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided.
COUPLING PROCESS FOR GENERATING REACTIVE BORON- CONTAINING DERIVATIVES OF N-SUBSTITUTED PYRROLE-2- CARBONITRILES TO PRODUCE BIARYLS
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Page/Page column 30-31, (2008/06/13)
A convenient preparation of boron-containing compounds, borate salts, pyrrolecarbonitrile boron-containing compounds, N-substituted-pyrrole-2-carbonitrile boron-containing compounds, and derivatives thereof is provided. The present invention also provides for the use of these boron-containing compounds and derivatives thereof in coupling reactions to provide bi-aryl compounds.
