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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 262295-11-4
分子式: C₂₁H₁₉F₆N₅O
分子量:471.41

保管条件:

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

Data Sheet (271 KB)

YM580 構造式

CAS 番号: 262295-11-4

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Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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)

体外実験

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

体内実験

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.}}

化学情報

CAS 番号 262295-11-4
分子量 471.41
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (271 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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