Org-31710 | CAS#118968-41-5 | Progesterone Receptor Antagonist

MedKoo Cat#: 528202 | Name: Org-31710

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Org-31710 is a progesterone receptor antagonist potentially for contraception. ORG-31710 induced transient up-regulation of inhibitor of apoptosis XIAP. The presence of swollen microvilli, precursors of endometrial pinopodes, was significantly reduced on cultures with Org 31710. The presence of Org 31710 significantly decreased the levels of PGE(2), PGF(2 alpha), and PA activity. These results suggest that P is essential in ovulation during the initial stages of the ovulatory process.

Chemical Structure

Org-31710

CAS#118968-41-5

Theoretical Analysis

MedKoo Cat#: 528202

Name: Org-31710

CAS#: 118968-41-5

Chemical Formula: C30H39NO2

Exact Mass: 445.2981

Molecular Weight: 445.65

Elemental Analysis: C, 80.86; H, 8.82; N, 3.14; O, 7.18

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

Org-31710; Org 31710; Org31710

IUPAC/Chemical Name

(6R,8S,11R,13S,14S,17R)-11-(4-(dimethylamino)phenyl)-6,13-dimethyl-1,4',5',6,7,8,11,12,13,14,15,16-dodecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3(2H)-one

InChi Key

HFDGABTZPISMDD-IEVXGSBISA-N

InChi Code

InChI=1S/C30H39NO2/c1-19-16-25-27-12-14-30(13-5-15-33-30)29(27,2)18-26(20-6-8-21(9-7-20)31(3)4)28(25)23-11-10-22(32)17-24(19)23/h6-9,17,19,25-27H,5,10-16,18H2,1-4H3/t19-,25+,26-,27+,29+,30+/m1/s1

SMILES Code

C[C@@]12[C@@]3(OCCC3)CC[C@@]1([H])[C@]4([H])C[C@@H](C)C5=CC(CCC5=C4[C@@H](C6=CC=C(N(C)C)C=C6)C2)=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

Shelf Life

>2 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

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 445.65 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: Goyeneche AA, Seidel EE, Telleria CM. Growth inhibition induced by antiprogestins RU-38486, ORG-31710, and CDB-2914 in ovarian cancer cells involves inhibition of cyclin dependent kinase 2. Invest New Drugs. 2012 Jun;30(3):967-80. doi: 10.1007/s10637-011-9655-z. PubMed PMID: 21424700; PubMed Central PMCID: PMC3348464. 2: Petersen A, Bentin-Ley U, Ravn V, Qvortrup K, Sørensen S, Islin H, Sjögren A, Mosselmann S, Hamberger L. The antiprogesterone Org 31710 inhibits human blastocyst-endometrial interactions in vitro. Fertil Steril. 2005 Apr;83 Suppl 1:1255-63. PubMed PMID: 15831300. 3: Mulders TM, Mink CP, Bobbink IW, Bennink HJ. Safety, tolerability, and pharmacokinetics of a novel, selective antiprogestagen (Org 31710) in healthy male volunteers. Contraception. 1998 Jul;58(1):39-44. PubMed PMID: 9743895. 4: van Heusden AM, Killick SR, Coelingh Bennink HJ, Fauser BC. Single monthly administration of the anti-progestagen Org 31710 in users of the 75 microg desogestrel progestagen-only pill: effects on pituitary-ovarian activity. Hum Reprod. 2000 Mar;15(3):629-36. PubMed PMID: 10686210. 5: Mizutani T, Bhakta A, Kloosterboer HJ, Moudgil VK. Novel antiprogestins Org 31806 and 31710: interaction with mammalian progesterone receptor and DNA binding of antisteroid receptor complexes. J Steroid Biochem Mol Biol. 1992 Aug;42(7):695-704. PubMed PMID: 1504008. 6: Svensson EC, Markström E, Shao R, Andersson M, Billig H. Progesterone receptor antagonists Org 31710 and RU 486 increase apoptosis in human periovulatory granulosa cells. Fertil Steril. 2001 Dec;76(6):1225-31. PubMed PMID: 11730755. 7: Pall M, Mikuni M, Mitsube K, Brännström M. Time-dependent ovulation inhibition of a selective progesterone-receptor antagonist (Org 31710) and effects on ovulatory mediators in the in vitro perfused rat ovary. Biol Reprod. 2000 Dec;63(6):1642-7. PubMed PMID: 11090431. 8: Kloosterboer HJ, Deckers GH, Schoonen WG. Pharmacology of two new very selective antiprogestagens: Org 31710 and Org 31806. Hum Reprod. 1994 Jun;9 Suppl 1:47-52. PubMed PMID: 7962469. 9: Kuo CT, Lee WS. Progesterone receptor activation is required for folic acid-induced anti-proliferation in colorectal cancer cell lines. Cancer Lett. 2016 Aug 10;378(2):104-10. doi: 10.1016/j.canlet.2016.05.019. PubMed PMID: 27233474. 10: Bylander A, Gunnarsson L, Shao R, Billig H, Larsson DG. Progesterone-mediated effects on gene expression and oocyte-cumulus complex transport in the mouse fallopian tube. Reprod Biol Endocrinol. 2015 May 13;13:40. doi: 10.1186/s12958-015-0038-8. PubMed PMID: 25967158; PubMed Central PMCID: PMC4450483. 11: Verbost PM, Hanssen RG, Korver GH, Mulders TM. ORG 33628 and ORG 31710 to control vaginal bleeding in progestin-only contraceptive regimens. Semin Reprod Med. 2005 Feb;23(1):101-11. Review. PubMed PMID: 15714394. 12: Kloosterboer HJ, Deckers GH, Schoonen WG, Hanssen RG, Rose UM, Verbost PM, Hsiu JG, Williams RF, Hodgen GD. Preclinical experience with two selective progesterone receptor modulators on breast and endometrium. Steroids. 2000 Oct-Nov;65(10-11):733-40. PubMed PMID: 11108884. 13: Hsu SP, Yang HC, Kuo CT, Wen HC, Chen LC, Huo YN, Lee WS. Progesterone receptor-NFκB complex formation is required for progesterone-induced NFκB nuclear translocation and binding onto the p53 promoter. Endocrinology. 2015 Jan;156(1):291-300. doi: 10.1210/en.2014-1629. PubMed PMID: 25353185. 14: Guzel E, Buchwalder L, Basar M, Kayisli U, Ocak N, Bozkurt I, Lockwood CJ, Schatz F. Effects of tibolone and its metabolites on prolactin and insulin-like growth factor binding protein-1 expression in human endometrial stromal cells. Gynecol Endocrinol. 2015 May;31(5):414-8. doi: 10.3109/09513590.2015.1014788. PubMed PMID: 25856298. 15: Gemzell-Danielsson K, van Heusden AM, Killick SR, Croxatto HB, Bouchard P, Cameron S, Bygdeman M. Improving cycle control in progestogen-only contraceptive pill users by intermittent treatment with a new anti-progestogen. Hum Reprod. 2002 Oct;17(10):2588-93. PubMed PMID: 12351534. 16: Hurd C, Underwood B, Herman M, Iwasaki K, Kloosterboer HJ, Dinda S, Moudgil VK. Characterization of ligand binding, DNA binding and phosphorylation of progesterone receptor by two novel progesterone receptor antagonist ligands. Mol Cell Biochem. 1997 Oct;175(1-2):205-12. PubMed PMID: 9350053. 17: Zheng S, Huang J, Zhou K, Xiang Q, Zhang Y, Tan Z, Simoncini T, Fu X, Wang T. Progesterone enhances vascular endothelial cell migration via activation of focal adhesion kinase. J Cell Mol Med. 2012 Feb;16(2):296-305. doi: 10.1111/j.1582-4934.2011.01305.x. PubMed PMID: 21418517; PubMed Central PMCID: PMC3823293. 18: Gamarra-Luques CD, Hapon MB, Goyeneche AA, Telleria CM. Resistance to cisplatin and paclitaxel does not affect the sensitivity of human ovarian cancer cells to antiprogestin-induced cytotoxicity. J Ovarian Res. 2014 Apr 27;7:45. doi: 10.1186/1757-2215-7-45. PubMed PMID: 24795781; PubMed Central PMCID: PMC4007005. 19: Kloosterboer HJ, Deckers GH, de Gooyer ME, Dijkema R, Orlemans EO, Schoonen WG. Pharmacological properties of a new selective antiprogestagen: Org 33628. Ann N Y Acad Sci. 1995 Jun 12;761:192-201. PubMed PMID: 7625721. 20: Klijn JG, Setyono-Han B, Sander HJ, Lamberts SW, de Jong FH, Deckers GH, Foekens JA. Pre-clinical and clinical treatment of breast cancer with antiprogestins. Hum Reprod. 1994 Jun;9 Suppl 1:181-9. Review. PubMed PMID: 7962463.