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Merck
CN

SML3084

Clascoterone

≥98% (HPLC)

Synonym(s):

21-Hydroxy-17-(1-oxopropoxy)pregn-4-ene-3,20-dione, C17P, CB-03-01, Cortexolone 17α-propionate

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About This Item

Empirical Formula (Hill Notation):
C24H34O5
CAS Number:
Molecular Weight:
402.52
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

CCC(O[C@]1(C(CO)=O)CC[C@@]2([H])[C@]3([H])CCC4=CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)=O

InChI

1S/C24H34O5/c1-4-21(28)29-24(20(27)14-25)12-9-19-17-6-5-15-13-16(26)7-10-22(15,2)18(17)8-11-23(19,24)3/h13,17-19,25H,4-12,14H2,1-3H3/t17-,18+,19+,22+,23+,24+/m1/s1

InChI key

GPNHMOZDMYNCPO-PDUMRIMRSA-N

Biochem/physiol Actions

Clascoterone is a high-affinity androgen receptor (AR) antagonist (antiandrogen) that antagonizes testosterone-stimulated transcription activity (in reporter cells) as well as DHT-induced production of lipids and inflammatory cytokines (in human sebocytes) in cultures. When applied topically, clascoterone is as active as cyproterone acetate, and 2-, 3-, and 4-times, respectively, more active than finasteride, flutamide, and progesterone in vivo (local antiandrogenic activity in hamster′s flank organ; 100-400 μg/50 μL acetone/animal).
High-affinity androgen receptor (AR) antagonist with antiandrogenic efficacy in vitro and in vivo.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Patrizia Ferraboschi et al.
Steroids, 128, 95-104 (2017-09-20)
Cortexolone-17α-propionate (CP) is a topically active antiandrogen useful in the treatment of skin disorders. In the solid state, three anhydrous forms of this drug (CPI, CPII and CPIII) occur, together with one hydrated crystal (CPW). The single crystal structure of
Caridad Rosette et al.
Journal of drugs in dermatology : JDD, 18(5), 412-418 (2019-05-31)
Cortexolone 17α-propionate (clascoterone) is a novel topical androgen antagonist that is being analyzed for its ability to treat acne. The pathogenesis of acne is attributed to multiple factors, including altered sebum production, inflammatory processes, dysregulation of the hormone microenvironment, and
Caridad Rosette et al.
Journal of drugs in dermatology : JDD, 18(2), 197-201 (2019-02-28)
Cortexolone 17α-propionate (clascoterone) is a novel androgen antagonist that is currently being analyzed in a large phase 2 clinical trial for the topical treatment of androgenetic alopecia (AGA). While the pathogenesis of AGA is still debated, the consensus is that



Global Trade Item Number

SKUGTIN
SML3084-25MG04065266519938
SML3084-5MG04065266519945