OP-3633

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

MedKoo CAT#: 555571

CAS#: 2102494-14-2

Description: 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

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OP-3633
CAS# 2102494-14-2
Instruction

Theoretical Analysis

MedKoo Cat#: 555571
Name: OP-3633
CAS#: 2102494-14-2
Chemical Formula: C30H39NO2
Exact Mass: 445.30
Molecular Weight: 445.647
Elemental Analysis: C, 80.86; H, 8.82; N, 3.14; O, 7.18

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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.

Biological target:
In vitro activity:
In vivo activity:

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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.