Tanaproget (Synonyms: NSP-989;NSP 989;NSP989) |
Katalog-Nr.GC16847
One-Click Copy Product Info
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Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 304853-42-7
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 304853-42-7 | SDF | |
| Überlieferungen | NSP-989;NSP 989;NSP989 | ||
| Chemical Name | 5-(4,4-dimethyl-2-sulfanylidene-1H-3,1-benzoxazin-6-yl)-1-methylpyrrole-2-carbonitrile | ||
| Canonical SMILES | CC1(C2=C(C=CC(=C2)C3=CC=C(N3C)C#N)NC(=S)O1)C | ||
| Formula | C16H15N3OS | M.Wt | 297.37 |
| Löslichkeit | DMSO : ≥ 50 mg/mL (168.14 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3628 mL | 16.8141 mL | 33.6281 mL |
| 5 mM | 672.6 μL | 3.3628 mL | 6.7256 mL |
| 10 mM | 336.3 μL | 1.6814 mL | 3.3628 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)