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YK11 Sale

目录号 : GC31442

A partial agonist of the androgen receptor

YK11 Chemical Structure

Cas No.:1370003-76-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥770.00
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5mg
¥438.00
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10mg
¥700.00
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50mg
¥840.00
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100mg
¥1,050.00
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Sample solution is provided at 25 µL, 10mM.

Description

YK-11 is an androgen receptor partial agonist that activates androgen receptor transcriptional activity in HEK293 cells overexpressing androgen receptors when used at a concentration of 0.1 μM.1 It induces expression of the androgen receptor target genes FKBP51 and FGF18 in HEK293 cells when used at a concentration of 10 μM. YK-11 accelerates nuclear translocation of androgen receptors without inducing interaction between the androgen receptor N- and C-termini. In C2C12 cells, YK-11 (500 nM) increases expression of the myogenic regulatory factors MyoD, Myf5, and myogenin, as well as follistatin (Fst), and induces myogenic differentiation.2 YK-11 also accelerates proliferation and mineralization and increases expression of the osteoblast differentiation markers osteoprotegerin and osteocalcin in MC3T3-E1 mouse osteoblast cells.3

1.Kanno, Y., Hikosaka, R., Zhang, S.-Y., et al.(17α,20E)-17,20-[(1-Methoxyethylidene)bis(oxy)]-3-oxo-19-norpregna-4,20-diene-21-carboxylic acid methyl ester (YK11) is a partial agonist of the androgen receptorBiol. Pharm. Bull.34(3)318-323(2011) 2.Kanno, Y., Ota, R., Someya, K., et al.Selective androgen receptor modulator, YK11, regulates myogenic differentiation of C2C12 myoblasts by follistatin expressionBiol. Pharm. Bull.36(9)1460-1465(2013) 3.Yatsu, T., Kusakabe, T., Kato, K., et al.Selective androgen receptor modulator, YK11, up-regulates osteoblastic proliferation and differentiation in MC3T3-E1 cellsBiol. Pharm. Bull.41(3)394-398(2018)

实验参考方法

Cell experiment:

Mouse myoblast C2C12 cells are cultured in Dulbecco’s modified Eagle’s medium (DMEM) supplemented with 10% fetal bovine serum (FBS) at 37°C in a humidified atmosphere with 5% CO2. C2C12 cells are seeded on plates and maintained in culture medium for 24 h. To induce myogenic differentiation, YK11 or DHT in DMEM supplemented with 2% horse serum (differentiation medium) is added to the cells on day 0. For the neutralization assay of Fst (also known as activin-binding protein), C2C12 cells are maintained in differentiation medium in the presence of anti-Fst antibody[1].

References:

[1]. Kanno Y, et al. Selective androgen receptor modulator, YK11, regulates myogenic differentiation of C2C12 myoblasts by follistatin expression. Biol Pharm Bull. 2013;36(9):1460-5.
[2]. Yatsu T, et al. Selective Androgen Receptor Modulator, YK11, Up-Regulates Osteoblastic Proliferation and Differentiation in MC3T3-E1 Cells. Biol Pharm Bull. 2018;41(3):394-398.

化学性质

Cas No. 1370003-76-1 SDF
Canonical SMILES O=C1CCC2C(CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@@]4(OC(C)(OC)O/5)C5=C/C(OC)=O)=C1
分子式 C25H34O6 分子量 430.53
溶解度 DMSO : ≥ 64 mg/mL (148.65 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.3227 mL 11.6136 mL 23.2272 mL
5 mM 0.4645 mL 2.3227 mL 4.6454 mL
10 mM 0.2323 mL 1.1614 mL 2.3227 mL
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