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Cat. No.: HY-180409

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YM580

YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC₅₀ = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and ERα (K_is > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer.

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CAS No.: 262295-11-4
Formule: C₂₁H₁₉F₆N₅O
Masse moléculaire:471.41

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

YM580 Chemical Structure

CAS No.: 262295-11-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & TargetAndrogen Receptor

hAR

4.6 nM (Ki)

rAR

6.2 nM (Ki)

rat PR

3300 nM (Ki)

human GR

>100000 nM (Ki)

human ERα

>100000 nM (Ki)

In Vitro

YM580 potently inhibits AR-mediated transcriptional activation in AR/CHO#3 cells, with an IC₅₀ of 0.11 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	Note	C_max	AUC_0-t	T_1/2	CL
Rat^[1]	3 nM	p.o.	plasma	702 ng/mL	21952 ng·h/mL	12.5 h	133 mL/h/kg
Rat^[1]	3 nM	p.o.	prostate	1561 ng/mL	43215 h·ng/g	11.2 h	68.3 mL/h/kg

In Vivo

YM580 (0.3-30 mg/kg; p.o.; daily; 15 days) reduces ventral prostate weight and exhibits antiandrogenic effect in mature intact male Wistar rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mature intact male Wistar rats (10-week-old)^[1]
Dosage:

0.3, 1, 3, 10, 30 mg/kg
Administration:

p.o.; daily; 15 days
Result:

Decreased ventral prostate weight in a dose-dependent manner with an ED_{50_{of 2.2 mg/kg/day, and an inhibition rate of 67% at 10 mg/kg/day.

Exerted a maximum antiandrogenic effect comparable to surgical castration at 30 mg/kg/day.

Did not significantly elevate serum testosterone levels across all doses.

Exhibited good peripheral selectivity.}}

Chemical Information

CAS No. 262295-11-4
Masse moléculaire 471.41
Formule C₂₁H₁₉F₆N₅O
SMILES

C[C@@H]1N(C2=CC(C(F)(F)F)=C(C#N)C=C2)C[C@@H](C)N(C(NC=3C=CC(C(F)(F)F)=NC3)=O)C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Kinoyama I, et al. (+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist. J Med Chem. 2006 Jan 26;49(2):716-26. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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