NSP989
- Product Name
- NSP989
- CAS No.
- 304853-42-7
- Chemical Name
- NSP989
- Synonyms
- NSP989;NSP 989;NSP-989;Tanaproget;Tanaproget (NSP989);NSP-989; NSP 989; NSP989;5-(1,4-dihydro-4,4-dimethyl-2-thioxo-2H-3,1-benzoxazin-6-yl)-1-methyl-1H-Pyrrole-2-carbonitrile;1H-Pyrrole-2-carbonitrile, 5-(1,4-dihydro-4,4-dimethyl-2-thioxo-2H-3,1-benzoxazin-6-yl)-1-methyl-;5-(4,4-dimethyl-2-thioxo-2,4-dihydro-1H-benzo[d][1,3]oxazin-6-yl)-1-methyl-1H-pyrrole-2-carbonitrile;5-(4,4-Dimethyl-2-thioxo-1,4-dihydro-2H-benzo[d][1,3]oxazin-6-yl)-1-methyl-1H-pyrrole-2-carbonitrile
- CBNumber
- CB52666690
- Molecular Formula
- C16H15N3OS
- Formula Weight
- 297.37
- MOL File
- 304853-42-7.mol
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)
- color
- Light yellow to yellow
- InChI
- 1S/C16H15N3OS/c1-16(2)12-8-10(4-6-13(12)18-15(21)20-16)14-7-5-11(9-17)19(14)3/h4-8H,1-3H3,(H,18,21)
- InChIKey
- PYVFWTPEBMRKSR-UHFFFAOYSA-N
- SMILES
- S=C1Nc2c(cc(cc2)c3[n](c(cc3)C#N)C)C(O1)(C)C
Safety
- Storage Class
- 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects - Hazard Classifications
- Repr. 1B
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..…
N-Bromosuccinimide Price
- Product number
- SML2779
- Product name
- Tanaproget
- Purity
- ≥98% (HPLC)
- Packaging
- 5 mg
- Price
- $128.25
- Updated
- 2025/07/31
- Product number
- SML2779
- Product name
- Tanaproget
- Purity
- ≥98% (HPLC)
- Packaging
- 25 mg
- Price
- $541
- Updated
- 2025/07/31
- Product number
- A3857
- Product name
- Tanaproget
- Packaging
- 2mg
- Price
- $245
- Updated
- 2021/12/16
- Product number
- A3857
- Product name
- Tanaproget
- Packaging
- 5mg
- Price
- $366
- Updated
- 2021/12/16
- Product number
- A3857
- Product name
- Tanaproget
- Packaging
- 10mg
- Price
- $520
- Updated
- 2021/12/16
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].
in vivo
Tanaproget (300 μg/kg; gavage/sustained-release capsules; once daily; 14-16 days) significantly reduces the number and size of human endometriotic lesions in the ncr/nude mouse endometriosis model[1].
Tanaproget (0.03 mg/kg; oral; once daily; 4 days) completely inhibits ovulation in the Sprague-Dawley rat ovulation inhibition model and is 30 times more potent than steroidal progestins[2].
| Animal Model: | Human endometriosis xenograft model in ncr/nude athymic mice (female, 5-week-old, ovariectomized)[1] |
| Dosage: | 300μg/kg (2% Tween 80/0.5% methylcellulose) |
| Administration: | Gavage or slow-release capsule, daily for 14–16 days |
| Result: | Reduced the number and size of human endometrial lesions derived from endometriosis patients, with complete regression in 33% of treated mice. |
| Animal Model: | Sprague-Dawley rats (female, 200 g, estrus-synchronized)[2] |
| Dosage: | 0.03 mg/kg (corn oil) |
| Administration: | Oral gavage, daily for 4 days |
| Result: | Completely inhibited ovulation in all treated rats at 0.03 mg/kg, showing 30-fold higher efficacy than medroxyprogesterone acetate (MPA). |
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.
NSP989 Preparation Products And Raw materials
Raw materials
Preparation Products
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