WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 200680
Description: Telapristone acetate, also known as CDB-4124 (proposed trade names Proellex and Progenta), is an investigational selective progesterone receptor modulator, tested for treatment of progesterone sensitive myomata. CDB-4124 was originally developed the National Institutes of Health, and as of 2012 is in Phase II clinical trials for uterine fibroids and endometriosis. It also has some antiglucocorticoid activity.
MedKoo Cat#: 200680
Name: Telapristone acetate
Chemical Formula: C31H39NO5
Exact Mass: 505.28282
Molecular Weight: 505.64
Elemental Analysis: C, 73.63; H, 7.77; N, 2.77; O, 15.82
Synonym: CDB4124; CDB-4124; CDB 4124; Telapristone acetate; brand name : Proellex Progenta
IUPAC/Chemical Name: (8S,11R,13S,14S,17R)-11-(4-(dimethylamino)phenyl)-17-(2-methoxyacetyl)-13-methyl-3-oxo-2,3,6,7,8,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate
InChi Key: JVBGZFRPTRKSBB-MJBQOYBXSA-N
InChi Code: InChI=1S/C31H39NO5/c1-19(33)37-31(28(35)18-36-5)15-14-27-25-12-8-21-16-23(34)11-13-24(21)29(25)26(17-30(27,31)2)20-6-9-22(10-7-20)32(3)4/h6-7,9-10,16,25-27H,8,11-15,17-18H2,1-5H3/t25-,26+,27-,30-,31-/m0/s1
SMILES Code: CC(O[C@]1(C(COC)=O)CC[C@@]2([H])[C@]3([H])CCC4=CC(CCC4=C3[C@@H](C5=CC=C(N(C)C)C=C5)C[C@]12C)=O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 505.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Spitz IM. Clinical utility of progesterone receptor modulators and their effect on the endometrium. Curr Opin Obstet Gynecol. 2009 Aug;21(4):318-24. Review. PubMed PMID: 19602929.
2: Ioffe OB, Zaino RJ, Mutter GL. Endometrial changes from short-term therapy with CDB-4124, a selective progesterone receptor modulator. Mod Pathol. 2009 Mar;22(3):450-9. Epub 2009 Jan 9. PubMed PMID: 19136935.
3: Benagiano G, Bastianelli C, Farris M. Selective progesterone receptor modulators 3: use in oncology, endocrinology and psychiatry. Expert Opin Pharmacother. 2008 Oct;9(14):2487-96. Review. PubMed PMID: 18778186.
4: Benagiano G, Bastianelli C, Farris M. Selective progesterone receptor modulators 2: use in reproductive medicine. Expert Opin Pharmacother. 2008 Oct;9(14):2473-85. PubMed PMID: 18778185.
5: Benagiano G, Bastianelli C, Farris M. Selective progesterone receptor modulators 1: use during pregnancy. Expert Opin Pharmacother. 2008 Oct;9(14):2459-72. Review. PubMed PMID: 18778184.
6: Leo JC, Lin VC. The activities of progesterone receptor isoform A and B are differentially modulated by their ligands in a gene-selective manner. Int J Cancer. 2008 Jan 1;122(1):230-43. PubMed PMID: 17893877.
7: Wiehle RD, Christov K, Mehta R. Anti-progestins suppress the growth of established tumors induced by 7,12-dimethylbenz(a)anthracene: comparison between RU486 and a new 21-substituted-19-nor-progestin. Oncol Rep. 2007 Jul;18(1):167-74. PubMed PMID: 17549364.
8: BayÃ©s M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Apr;27(3):193-219. PubMed PMID: 15834452.
9: Attardi BJ, Burgenson J, Hild SA, Reel JR. In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88. PubMed PMID: 15120421.
10: Attardi BJ, Burgenson J, Hild SA, Reel JR, Blye RP. CDB-4124 and its putative monodemethylated metabolite, CDB-4453, are potent antiprogestins with reduced antiglucocorticoid activity: in vitro comparison to mifepristone and CDB-2914. Mol Cell Endocrinol. 2002 Feb 25;188(1-2):111-23. PubMed PMID: 11911951.
CDB-4124 (proposed trade names Proellex, Progenta) is an investigational selective progesterone receptor modulator, tested for treatment of progesterone sensitive myomata. As of September 2008, it is undergoing Phase II and III clinical trials.