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Merck
CN

SML3084

Clascoterone

≥98% (HPLC)

别名:

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

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关于此项目

经验公式(希尔记法):
C24H34O5
化学文摘社编号:
分子量:
402.52
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
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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

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 key

GPNHMOZDMYNCPO-PDUMRIMRSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

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.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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Cortexolone 17α-propionate for hidradenitis suppurativa.
Samuel Antranig Der Sarkissian et al.
Dermatologic therapy, 33(6), e14142-e14142 (2020-08-08)
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
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
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

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