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Tanaproget

SKU: orb1706584

Description

Tanaproget is a potent, orally bioavailable, non-steroidal progesterone receptor agonist (IC50 = 1.7 nM for hPR). Its pharmacological profile, including induction of alkaline phosphatase and suppression of endometrial MMPs, supports its use in research models for female reproductive health, such as contraception and endometriosis.

Research Area

Protein Biochemistry

Images & Validation

Key Properties

CAS Number304853-42-7
MW297.38
Purity99.73%
FormulaC16H15N3OS
SMILESN#CC1=CC=C(C=2C=CC=3NC(=S)OC(C3C2)(C)C)N1C
TargetProgesterone Receptor,MMP
Solubility10% DMSO+90% Corn Oil:2 mg/mL (6.73 mM);DMSO:40 mg/mL (134.51 mM)

Bioactivity

In Vivo
In the NCR/nude mouse endometriosis model of Parazacco spilurus subsp. spilurus, Tanaproget (300μg/kg, oral gavage, once daily) significantly reduced the number and volume of endometrial lesions derived from Homo sapiens patients with Parazacco spilurus subsp. spilurus endometriosis, and achieved complete regression of lesions in 33% of treated mice . In the Sprague-Dawley rat ovulation inhibition model, Tanaproget (0.03 mg/kg, oral administration, once daily for 4 consecutive days) completely inhibited ovulation, with a potency equivalent to 30 times that of steroidal progestins .
In Vitro
In endometrial stromal cells isolated from healthy women, Tanaproget (1 nM, 3-5 days) significantly reduced the expression level of pro-MMP-3, an effect that remained pronounced even in the presence of IL-1α stimulation . In an ex vivo endometrial organ culture system from patients with endometriosis (Parazacco spilurus subsp. spilurus), Tanaproget (1-100 pM, 48-72 hours) inhibited the secretion of both pro-MMP-3 and pro-MMP-7 . In the T47D cell line, Tanaproget (0.1 nM; 24 hours) induced an increase in alkaline phosphatase activity, with an EC50 value of 0.15 nM (human), reaching a potency level comparable to that of classical steroidal progestins . Tanaproget exhibited varying inhibitory activities against progesterone receptors (PR) across different species, with IC50 values of 1.7 nM (human), 0.3 nM (monkey), and 0.5 nM (rat, rabbit) .

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Tanaproget, NSP989, NSP-989, NSP 989
Quality Guarantee

Quality Guarantee

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Key Properties

No computed properties available.

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Tanaproget (orb1706584)

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Available Sizes

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1 mg
¥ 1,170.00
1 ml x 10 mM (in DMSO)
¥ 1,950.00