NSP989 Property

Melting point:

225-228℃

Boiling point:

441.3±55.0 °C(Predicted)

Density 

1.26±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Powder

pka

11.84±0.40(Predicted)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H360May damage fertility or the unborn child

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P501Dispose of contents/container to..…

NSP989 Chemical Properties,Usage,Production

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].

target

progesterone receptor

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.