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Tanaproget (Synonyms: NSP-989)

Cat. No.: HY-15606 Purity: 99.93%
Handling Instructions

Tanaproget (NSP-989) is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins.

For research use only. We do not sell to patients.

Tanaproget Chemical Structure

Tanaproget Chemical Structure

CAS No. : 304853-42-7

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Solution
10 mM * 1 mL in DMSO USD 264 In-stock
Estimated Time of Arrival: December 31
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10 mM * 1 mL
ready for reconstitution
USD 264 In-stock
Estimated Time of Arrival: December 31
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5 mg USD 240 In-stock
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10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Tanaproget (NSP-989) is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins. IC50 value: 0.1 nM (EC50, induce alkaline phosphatase activity) [1] Target: progesterone receptor Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives. in vitro: In T47D cells, TNPR induces alkaline phosphatase activity with an EC(50) value of 0.1 nm, comparable with potent steroidal progestins such as medroxyprogesterone acetate (MPA) and trimegestone (TMG), albeit with a reduced efficacy ( approximately 60%). In a mammalian two-hybrid assay to measure PR agonist-induced interaction between steroid receptor co-activator-1 and PR, TNPR showed similar potency (EC(50) value of 0.02 nm) and efficacy to MPA and TMG [1]. in vivo: TNPR effectively down-regulated MMP expression in vitro and induced significant reduction of lesions in mice with disease established by tissues from endometriosis patients [2]. The maximum concentration (C(max)) of tanaproget occurred approximately 2 to 3 h after administration. The elimination half-life (t(1/2)) ranged from 12 to 30 h, and the oral clearance was approximately 70 L/h. The pharmacokinetics of tanaproget was not noticeably altered with a high-fat meal [3]. Toxicity: All doses of tanaproget decreased cervical mucus scores (using a modified Insler method), indicating poor production and poor quality of cervical mucus. The most frequent treatment-emergent adverse events were vaginal bleeding/spotting, abdominal cramping and vomiting; their incidence was not dose related and most events were mild [3].

Molecular Weight

297.37

Formula

C₁₆H₁₅N₃OS

CAS No.
SMILES

N#CC1=CC=C(C2=CC=C(NC(OC3(C)C)=S)C3=C2)N1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (168.14 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
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Keywords:

TanaprogetNSP-989NSP989NSP 989Progesterone ReceptorNR3C3Inhibitorinhibitorinhibit

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Tanaproget
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HY-15606
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