Rogletimide

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

MedKoo CAT#: 461129

CAS#: 92788-10-8

Description: Rogletimide is a selective aromatase inhibitor. Rogletimide is related to the drug aminoglutethimide, but with no significant sedative effect. It potentially useful in the treatment of some forms of cancer.

Chemical Structure

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Rogletimide
CAS# 92788-10-8
Instruction

Theoretical Analysis

MedKoo Cat#: 461129
Name: Rogletimide
CAS#: 92788-10-8
Chemical Formula: C12H14N2O2
Exact Mass: 218.11
Molecular Weight: 218.250
Elemental Analysis: C, 66.04; H, 6.47; N, 12.84; O, 14.66

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.

Request quote for custom synthesis

Synonym: Rogletimide; 3-PYG; 3 PYG; 3PYG; Pyridoglutethimide;

IUPAC/Chemical Name: (R)-3-ethyl-3-(pyridin-4-yl)piperidine-2,6-dione

InChi Key: QXKJWHWUDVQATH-GFCCVEGCSA-N

InChi Code: InChI=1S/C12H14N2O2/c1-2-12(9-4-7-13-8-5-9)6-3-10(15)14-11(12)16/h4-5,7-8H,2-3,6H2,1H3,(H,14,15,16)/t12-/m1/s1

SMILES Code: O=C(CC1)NC([C@@]1(CC)c2ccncc2)=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: >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: 2934.99.03.00

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 218.25 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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2: Newton CJ, Mehta A, Dowsett M. The effect of the aromatase inhibitor, rogletimide (pyridoglutethimide), on guinea pig adrenal cell steroidogenesis and placental microsomal aromatase activity: comparison with aminoglutethimide and CGS 16949A. J Steroid Biochem Mol Biol. 1991 Nov;39(5A):723-7. PubMed PMID: 1659868.

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8: Ogbunude PO, Aboul-Enein HY. In vitro inhibition of aromatase by the enantiomers of aminoglutethimide and analogs. Chirality. 1994;6(8):623-6. PubMed PMID: 7857773.

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15: Dowsett M, MacNeill F, Mehta A, Newton C, Haynes B, Jones A, Jarman M, Lonning P, Powles TJ, Coombes RC. Endocrine, pharmacokinetic and clinical studies of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione ('pyridoglutethimide') in postmenopausal breast cancer patients. Br J Cancer. 1991 Nov;64(5):887-94. PubMed PMID: 1931611; PubMed Central PMCID: PMC1977449.

16: Kelloff GJ, Lubet RA, Lieberman R, Eisenhauer K, Steele VE, Crowell JA, Hawk ET, Boone CW, Sigman CC. Aromatase inhibitors as potential cancer chemopreventives. Cancer Epidemiol Biomarkers Prev. 1998 Jan;7(1):65-78. Review. PubMed PMID: 9456245.

17: Aboul-Enein HY, Serignese V, Minguillón C, Oliveros L. Enantioselective separation of several piperidine-2, 6-diones on a covalently bonded cellulose 3,5-dimethylphenyl carbamate/10-undecenoate chiral selector. Biomed Chromatogr. 1997 Sep-Oct;11(5):303-6. Erratum in: Biomed Chromatogr 1998 Jan-Feb;12(1):45. PubMed PMID: 9376714.

18: Lønning PE, Dowsett M, Powles TJ. Postmenopausal estrogen synthesis and metabolism: alterations caused by aromatase inhibitors used for the treatment of breast cancer. J Steroid Biochem. 1990 Mar;35(3-4):355-66. Review. PubMed PMID: 2139151.

19: Dowsett M. Clinical development of aromatase inhibitors for the treatment of breast and prostate cancer. J Steroid Biochem Mol Biol. 1990 Dec 20;37(6):1037-41. Review. PubMed PMID: 2149504.

20: Yamamoto T, Urabe M, Tamura T, Kitawaki J, Honjo H, Okada H. Antitumor effect of pyridoglutethimide, an aromatase inhibitor, on 7,12-dimethylbenz(a)anthracene-induced mammary tumors of rat. Anticancer Res. 1991 Nov-Dec;11(6):1999-2002. PubMed PMID: 1776832.