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Purity: ≥98%
YK-11 is a novel, potent, synthetic, steroidal selective androgen receptor modulator (SARM) with osteogenic activity that functions as a partial agonist of the androgen receptor. Without requiring the N/C interaction, YK11 triggers AR. In the presence of YK11 as opposed to DHT, there was a greater induction of important myogenic regulatory factors (MRFs), including myogenic differentiation factor (MyoD), myogenic factor 5 (Myf5), and myogenin. Follistatin (Fst) expression was induced by YK11 treatment of C2C12 cells, but not by DHT. Anti-Fst antibody was able to reverse the YK11-mediated myogenic differentiation. These findings imply that YK11's anabolic effect depends on the induction of Fst. It is a partial agonist of the androgen receptor (AR) that is selective for specific genes and does not cause the N/C interaction, or the physical interaction between the NTD/AF1 and LBD/AF2, which is necessary for the full transactivation of the AR.
| Targets |
Androgen receptor
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| ln Vitro |
By upregulating Fst mRNA via AR at 500 nM, YK11, a partial agonist of androgen acquisition, causes myogenic secretion in C2C12 cells. Although it needs to be at high doses (100 nM or 500 nM), YK11 increases the expression of Myf5 and Myogenin mRNA [1]. YK11 (0.5 μM) stimulates osteoblast MC3T3-E1 cell proliferation and amplifies ALP activity via AR. Additionally, YK11 boosts the quantitative expression of osteocalcin mRNA (0.1-1.0 μM) and osteoprotegerin mRNA (0.5 μM). Furthermore, YK11 uses quick non-genomic signaling to increase the phosphorylation of the Akt protein [2].
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| Animal Protocol |
Mouse myoblast C2C12 cells are cultivated at 37°C in a humidified environment with 5% CO2 in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS). After being seeded onto plates, C2C12 cells are kept alive for 24 hours in culture medium. On day 0, the cells are treated with YK11 or DHT in DMEM supplemented with 2% horse serum (differentiation medium) to induce myogenic differentiation. Fst, also referred to as activin-binding protein, is neutralized in an assay where C2C12 cells are cultured in differentiation medium with anti-Fst antibody present[1].
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| 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 |
| Molecular Formula |
C25H34O6
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| Molecular Weight |
430.54
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| Exact Mass |
430.24
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| Elemental Analysis |
C, 69.74; H, 7.96; O, 22.30
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| CAS # |
1370003-76-1
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@]24/C(=C\C(=O)OC)/OC(O4)(C)OC)CCC5=CC(=O)CC[C@H]35
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| InChi Key |
KCQHQCDHFVGNMK-PQUNLUOYSA-N
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| InChi Code |
InChI=1S/C25H34O6/c1-23-11-9-18-17-8-6-16(26)13-15(17)5-7-19(18)20(23)10-12-25(23)21(14-22(27)28-3)30-24(2,29-4)31-25/h13-14,17-20H,5-12H2,1-4H3/b21-14+/t17-,18+,19+,20-,23-,24?,25+/m0/s1
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| Chemical Name |
methyl (2E)-2-[(8R,9S,10R,13S,14S,17S)-2'-methoxy-2',13-dimethyl-3-oxospiro[1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-17,5'-1,3-dioxolane]-4'-ylidene]acetate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3227 mL | 11.6133 mL | 23.2266 mL | |
| 5 mM | 0.4645 mL | 2.3227 mL | 4.6453 mL | |
| 10 mM | 0.2323 mL | 1.1613 mL | 2.3227 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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