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product name Ulipristal


Description: Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure. Ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. It also binds to the glucocorticoid receptor, but has no relevant affinity to the estrogen, androgen and mineralocorticoid receptors. Ulipristal acetate dose dependently suppressed progesterone-induced acrosome reaction and hyperactivation in human spermatozoa.

References: J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88; Clin Ther. 2012 Jan;34(1):24-36. 



Molecular Weight (MW)

433.58 
Formula

C28H35NO3 
CAS No.

159811-51-5 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 83 mg/mL (191.4 mM) 
Water: <1 mg/mL
Ethanol: 14 mg/mL (32.3 mM) 
Solubility (In vivo)

 
Synonyms

CDB-2914 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19419201

In Vitro

In vitro activity: Ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. It also binds to theglucocorticoid receptor, but has no relevant affinity to the estrogen, androgen and mineralocorticoid receptors.


Kinase Assay:


Cell Assay

In Vivo Based on clinical trials, ulipristal acetate seems to be a reasonably tolerable and effective method of emergency contraception when used within 120 hours of intercourse. Ulipristal acetate is at least as effective as LNG when used within the first 72 hours after unprotected intercourse. However, ulipristal acetate may be more effective than LNG when used between 72 to 120 hours after unprotected intercourse, extending the window of opportunity for emergency contraception. 
Animal model  
Formulation & Dosage  
References J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88; Clin Ther. 2012 Jan;34(1):24-36.  

GSK2606415

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Author: Sodium channel