CAS 595-33-5|Megestrol acetate

Introduction：Basic information about CAS 595-33-5|Megestrol acetate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Megestrol acetate BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
MUTATION DATA
5. Safety Information
6. Articles6
7. Synonyms

Common Name	Megestrol acetate
CAS Number	595-33-5	Molecular Weight	384.509
Density	1.2±0.1 g/cm3	Boiling Point	507.1±50.0 °C at 760 mmHg
Molecular Formula	C₂₄H₃₂O₄	Melting Point	214°C
MSDS	ChineseUSA	Flash Point	218.5±30.2 °C
Symbol	GHS08	Signal Word	Warning

Names

Name	megestrol acetate
Synonym	More Synonyms

Megestrol acetate BiologicalActivity

Description	Megestrol Acetate is a synthetic progesteronal agent with an IC50 of 260 μM for the inhibition of HegG2.Target: Progesterone ReceptorMegestrol acetate, also known as 17α-acetoxy-6-dehydro-6-methylprogesterone, and sometimes abbreviated as MGA or MA, is a steroidal progestin and progesterone derivative (specifically, a 17-hydroxylated progesterone) with predominantly progestational and antigonadotropic effects. Megestrol acetate is a good candidate for muscle wasting treatment and future studies addressed at the interaction between the drug and protein turnover in human skeletal muscle should be performed.
Related Catalog	Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Others >>Progesterone ReceptorResearch Areas >>Endocrinology
References	[1]. Neumann, F., The physiological action of progesterone and the pharmacological effects of progestogens--a short review. Postgrad Med J, 1978. 54 Suppl 2: p. 11-24. [2]. Argiles, J.M., A. Anguera, and B. Stemmler, A new look at an old drug for the treatment of cancer cachexia: megestrol acetate. Clin Nutr, 2013. 32(3): p. 319-24.

Description

Megestrol Acetate is a synthetic progesteronal agent with an IC50 of 260 μM for the inhibition of HegG2.Target: Progesterone ReceptorMegestrol acetate, also known as 17α-acetoxy-6-dehydro-6-methylprogesterone, and sometimes abbreviated as MGA or MA, is a steroidal progestin and progesterone derivative (specifically, a 17-hydroxylated progesterone) with predominantly progestational and antigonadotropic effects. Megestrol acetate is a good candidate for muscle wasting treatment and future studies addressed at the interaction between the drug and protein turnover in human skeletal muscle should be performed.

Related Catalog

Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Others >>Progesterone ReceptorResearch Areas >>Endocrinology

References

[1]. Neumann, F., The physiological action of progesterone and the pharmacological effects of progestogens--a short review. Postgrad Med J, 1978. 54 Suppl 2: p. 11-24.

[2]. Argiles, J.M., A. Anguera, and B. Stemmler, A new look at an old drug for the treatment of cancer cachexia: megestrol acetate. Clin Nutr, 2013. 32(3): p. 319-24.

Chemical & Physical Properties

Density	1.2±0.1 g/cm3
Boiling Point	507.1±50.0 °C at 760 mmHg
Melting Point	214°C
Molecular Formula	C₂₄H₃₂O₄
Molecular Weight	384.509
Flash Point	218.5±30.2 °C
Exact Mass	384.230072
PSA	60.44000
LogP	3.82
Vapour Pressure	0.0±1.3 mmHg at 25°C
Index of Refraction	1.551
InChIKey	RQZAXGRLVPAYTJ-GQFGMJRRSA-N
SMILES	CC(=O)OC1(C(C)=O)CCC2C3C=C(C)C4=CC(=O)CCC4(C)C3CCC21C
Storage condition	Refrigerator

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TU4075000

CHEMICAL NAME :: Pregna-4,6-diene-3,20-dione, 17-hydroxy-6-methyl-, acetate

CAS REGISTRY NUMBER :: 595-33-5

LAST UPDATED :: 199806

DATA ITEMS CITED :: 40

MOLECULAR FORMULA :: C24-H32-O4

MOLECULAR WEIGHT :: 384.56

WISWESSER LINE NOTATION :: L E5 B666 OV KU MUTJ A1 E1 FV1 FOV1 L1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 56 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 256 mg/kg/7Y-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Skin and Appendages - tumors Endocrine - diabetes mellitus

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 182 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Skin and Appendages - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 210 ug/kg

SEX/DURATION :: female 21 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1825 ug/kg

SEX/DURATION :: female 52 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2430 ug/kg

SEX/DURATION :: female 34 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1820 ug/kg

SEX/DURATION :: female 26 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 1800 ug/kg

SEX/DURATION :: female 30 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 1440 ug/kg

SEX/DURATION :: female 43 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 1440 ug/kg

SEX/DURATION :: female 40 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 1840 ug/kg

SEX/DURATION :: female 43 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1200 mg/kg

SEX/DURATION :: male 30 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2790 ug/kg

SEX/DURATION :: female 50 week(s) pre-mating female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 9 mg/kg

SEX/DURATION :: female 15-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 15 mg/kg

SEX/DURATION :: male 15 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 15 mg/kg

SEX/DURATION :: female 15 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 140 mg/kg

SEX/DURATION :: female 1-7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 7 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 70 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 14 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 15 mg/kg

SEX/DURATION :: female 30 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3 mg/kg

SEX/DURATION :: female 3 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 16800 ug/kg

SEX/DURATION :: female 21 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4600 ug/kg

SEX/DURATION :: female 23 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina Reproductive - Maternal Effects - other effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 100 ug/kg

SEX/DURATION :: female 5 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2 mg/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 625 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - mating performance (e.g. # sperm positive females per # females mated; # copulations per # estrus cycles)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 150 ug/kg

SEX/DURATION :: female 3 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 37500 ng/kg

SEX/DURATION :: female 3 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 50 ug/kg

SEX/DURATION :: female 5 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 128 ug/kg

SEX/DURATION :: female 16 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

TYPE OF TEST :: DNA adduct

TYPE OF TEST :: Unscheduled DNA synthesis

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

REFERENCE :: JOENAK Journal of Endocrinology. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1939- Volume(issue)/page/year: 60,167,1974 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 21,431,1979 TOXICOLOGY REVIEW CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,309,1976 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6284 No. of Facilities: 22 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 771 (estimated) No. of Female Employees: 372 (estimated)

Safety Information

Symbol	GHS08
Signal Word	Warning
Hazard Statements	H351-H373
Precautionary Statements	P281
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xn:Harmful
Risk Phrases	R40;R48
Safety Phrases	S22-S24/25
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	TU4075000

Articles6

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

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There are many of pathogen parasite species with different susceptibility profile to antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one pa...

Synonyms

(8R,9S,10R,13S,14S,17R)-17-Acetyl-6,10,13-trimethyl-3-oxo-2,3,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylacetat

Megestil

Pregna-4,6-diene-3,20-dione, 17-hydroxy-6-methyl-, acetate

Megestin

Pruritex Chat

Felipil

Nuvacon

6-Dehydro-6-methyl-17a-acetoxyprogesterone

Citestrol

Megace

Pregna-4,6-diene-3,20-dione, 17-(acetyloxy)-6-methyl-, (9β,10α)-

Megoestrolacetat

Megostat

6-Methyl-3,20-dioxopregna-4,6-dien-17-yl acetate

Megestrol acetate

Megestrol acetate [USAN]

17α-Acetoxy-6-methylpregna-4,6-diene-3,20-dione

Megestrol 17-acetate

Pill'Kan

Estropill

Kombiquens

Megefren

EINECS 209-864-5

17α-Acetoxy-6-methyl-4,6-pregnadiene-3,20-dione

Maygace

Volidan

6-Methyl-D4,6-pregnadien-17a-ol-3,20-dione Acetate

Pregna-4,6-diene-3,20-dione, 17-(acetyloxy)-6-methyl-

17a-Acetoxy-6-methylpregna-4,6-diene-3,20-dione

Minigest

Megestryl acetate

Nia

acétate de (8R,9S,10R,13S,14S,17R)-17-acétyl-6,10,13-triméthyl-3-oxo-2,3,8,9,10,11,12,13,14,15,16,17-dodécahydro-1H-cyclopenta[a]phénanthrén-17-yle

6-Dehydro-6-methyl-17α-acetoxyprogesterone

Opochaleurs

Suppress

[(8R,9S,10R,13S,14S,17R)-17-acetyl-6,10,13-trimethyl-3-oxo-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate

Megecat

Volplan

Progesterone, 6-dehydro-17-hydroxy-6-methyl-, acetate

Pilucalm

MFCD00056470

Gorda

Canipil

(8R,9S,10R,13S,14S,17R)-17-acetyl-6,10,13-trimethyl-3-oxo-2,3,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate

Megestrol (Acetate)

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