OP-3633 |CAS#2102494-14-2 | GR antagonist

MedKoo Cat#: 555571 | Name: OP-3633

Description:

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

OP-3633 is a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (IC50 = 29 nM). OP-3633 emerged as a glucocorticoid receptor (GR) antagonist with increased selectivity against PR and AR, improved cytochrome P450 inhibition profile, and significantly improved pharmacokinetic properties. OP-3633 demonstrated substantial inhibition of GR transcriptional activity in the GR positive HCC1806 triple negative breast cancer xenograft model. Overall, OP-3633 is a promising GR antagonist candidate to clinically evaluate the impact of GR inhibition in reversal or prevention of therapy resistance.

Chemical Structure

OP-3633

CAS#2102494-14-2

Theoretical Analysis

MedKoo Cat#: 555571

Name: OP-3633

CAS#: 2102494-14-2

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.

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Related CAS #

No Data

Synonym

OP-3633; OP 3633; OP3633;

IUPAC/Chemical Name

(8S,9R,10R,11S,13S,14S,17S)-11-(4-(Dimethylamino)-phenyl)-17-hydroxy-10,13-dimethyl-17-(prop-1-yn-1-yl)-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3Hcyclopenta[a]phenanthren-3-one

InChi Key

LJUSMSPTDKGAFT-LMNHVJTASA-N

InChi Code

InChI=1S/C30H39NO2/c1-6-15-30(33)17-14-26-24-12-9-21-18-23(32)13-16-28(21,2)27(24)25(19-29(26,30)3)20-7-10-22(11-8-20)31(4)5/h7-8,10-11,18,24-27,33H,9,12-14,16-17,19H2,1-5H3/t24-,25+,26-,27+,28-,29-,30-/m0/s1

SMILES Code

O=C1CC[C@]2(C)[C@@]3([H])[C@@H](C4=CC=C(N(C)C)C=C4)C[C@]5(C)[C@@](C#CC)(O)CC[C@@]5([H])[C@]3([H])CCC2=C1

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

>3 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

The glucocorticoid receptor (GR) is a member of the superfamily of nuclear hormone receptors that are activated by both natural and synthetic glucocorticoids (GCs), such as cortisol and dexamethasone, respectively. Given the plethora of biological processes regulated by GCs, dysregulation in receptor signaling has been implicated in a number of disease states including Cushing’s syndrome, diabetes depression, cancer, and immunosuppression. Accordingly, there has been considerable interest in the development of GR antagonists for therapeutic purposes.

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: Du X, Eksterowicz J, Zhou H, Rew Y, Zhu L, Yan X, Medina JC, Huang T, Chen X, Sutimantanapi D, Jahchan N, Kong W, Sun J, Zavorotinskaya T, Ye Q, Fantin VR, Sun D. Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633). J Med Chem. 2019 Jul 5. doi: 10.1021/acs.jmedchem.9b00711. [Epub ahead of print] PubMed PMID: 31274313.