| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Tanaproget targets the progesterone receptor (PR), a member of the nuclear receptor superfamily. It is a nonsteroidal PR agonist that binds to PR from various species with high affinity. It promotes the interaction between PR receptors and coactivators such as SRC-1, thereby inhibiting the secretion of matrix metalloproteinases (MMP-3/MMP-7) and reducing endometrial tissue invasion and angiogenesis.
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| ln Vitro |
In vitro, Tanaproget induces alkaline phosphatase activity in T47D cells with an EC50 of 0.15 nM (human). It significantly reduces pro-MMP-3 expression levels in endometrial stromal cells isolated from normal women at 1 nM for 3-5 days. It inhibits pro-MMP-3 and pro-MMP-7 secretion in endometrial organ cultures from endometriosis patients at 1-100 pM for 48-72 hours. Its IC50 values for PR from different species are 1.7 nM (human), 0.3 nM (monkey), and 0.5 nM (rat, rabbit).
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| ln Vivo |
In vivo, Tanaproget significantly reduces the number and volume of human endometrial lesions in an endometriosis mouse model at 300 μg/kg (p.o., daily). In a rat ovulation inhibition model, it completely inhibits ovulation at 0.03 mg/kg (p.o., daily for 4 days), with 30 times the potency of steroidal progestins.
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| Enzyme Assay |
In vitro receptor binding assays for Tanaproget involve measuring affinity for the progesterone receptor. Cytosolic preparations from cells expressing human PR are incubated with radiolabeled ligands and varying concentrations of Tanaproget. Non-specific binding is determined in the presence of excess unlabeled ligand. Bound radioactivity is collected by filtration and quantified by scintillation counting. IC50 values are calculated from competition curves.
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| Cell Assay |
For in vitro cell-based assays, T47D cells are cultured and treated with Tanaproget at various concentrations (e.g., 0.1 nM for 24 hours). Alkaline phosphatase activity is measured using a colorimetric assay. Endometrial stromal cells are treated with Tanaproget (1 nM, 3-5 days), and MMP-3 expression is measured by Western blot or ELISA. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo animal studies for Tanaproget use a nude mouse endometriosis model. Mice are implanted with human endometrial tissue, and Tanaproget is administered orally at 300 μg/kg daily. Lesion number and volume are measured. In a rat ovulation inhibition model, Sprague-Dawley rats are treated orally with 0.03 mg/kg Tanaproget daily for 4 days, and ovulation is assessed.
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| ADME/Pharmacokinetics |
Tanaproget (CAS 304853-42-7) has a molecular formula of C16H15N3OS and a molecular weight of 297.38. It is a yellow solid. It is soluble in DMSO. For in vivo formulation, it can be prepared in appropriate vehicles. Detailed pharmacokinetic parameters are not extensively characterized in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Tanaproget are not extensively provided. As a PR agonist, it would be expected to have a safety profile related to hormonal modulation. The compound is for research use only and is not for human or clinical use. Standard toxicology assessments would be required for therapeutic development.
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| References |
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| Additional Infomation |
Tanaproget (NSP-989) is an investigational nonsteroidal progestin. It is a high-affinity, highly potent progesterone receptor (PR) agonist with higher binding selectivity compared to most conventional progestins. Therefore, Tanaproget may have fewer side effects. Currently, Ligand Pharmaceuticals is developing Tanaproget as a clinical contraceptive. The Tanaproget analogue 4-fluoropropylTanaproget (18F) has been developed as a radiotracer for PR imaging in positron emission tomography (PET).
Tanaproget (NSP-989) is a novel nonsteroidal progesterone receptor agonist that is first in its class and has high affinity and selectivity for the progesterone receptor. It has been studied for its potential in contraception and endometriosis. No approved therapeutic status is reported. |
| Molecular Formula |
C16H15N3OS
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|---|---|
| Molecular Weight |
297.3748
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| Exact Mass |
297.094
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| Elemental Analysis |
C, 64.62; H, 5.08; N, 14.13; O, 5.38; S, 10.78
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| CAS # |
304853-42-7
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| Related CAS # |
304853-42-7
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| PubChem CID |
4369524
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.181
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
483
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N#CC1=CC=C(C2=CC=C(NC(OC3(C)C)=S)C3=C2)N1C
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| InChi Key |
PYVFWTPEBMRKSR-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
5-(4,4-dimethyl-2-sulfanylidene-1H-3,1-benzoxazin-6-yl)-1-methylpyrrole-2-carbonitrile
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| Synonyms |
Tanaproget; NSP 989; NSP-989; NSP989
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (~168.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3628 mL | 16.8141 mL | 33.6281 mL | |
| 5 mM | 0.6726 mL | 3.3628 mL | 6.7256 mL | |
| 10 mM | 0.3363 mL | 1.6814 mL | 3.3628 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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