YK11
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MedKoo CAT#: 530400

CAS#: 1370003-76-1

Description: YK-11 is a synthetic, steroidal selective androgen receptor modulator (SARM). It is a gene-selective partial agonist of the androgen receptor (AR) and does not induce the physical interaction between the NTD/AF1 and LBD/AF2 (known as the N/C interaction), which is required for full transactivation of the AR. The drug has anabolic activity in vitro in C2C12 myoblasts and shows greater potency than dihydrotestosterone (DHT) in this regard.


Chemical Structure

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YK11
CAS# 1370003-76-1

Theoretical Analysis

MedKoo Cat#: 530400
Name: YK11
CAS#: 1370003-76-1
Chemical Formula: C25H34O6
Exact Mass: 430.2355
Molecular Weight: 430.541
Elemental Analysis: C, 69.74; H, 7.96; O, 22.30

Price and Availability

Size Price Availability Quantity
25.0mg USD 90.0 Ready to ship
50.0mg USD 150.0 Ready to ship
100.0mg USD 250.0 Ready to ship
500.0mg USD 550.0 Ready to ship
1.0g USD 950.0 Ready to ship
2.0g USD 1650.0 Ready to ship
5.0g USD 3450.0 Ready to ship
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Synonym: YK-11; YK 11; YK11.

IUPAC/Chemical Name: methyl (E)-2-((8R,9S,10R,13S,14S,17R)-2'-methoxy-2',13-dimethyl-3-oxo-1,2,3,6,7,8,9,10,11,12,13,14,15,16-tetradecahydrospiro[cyclopenta[a]phenanthrene-17,4'-[1,3]dioxolan]-5'-ylidene)acetate

InChi Key: KCQHQCDHFVGNMK-DEIKBOPOSA-N

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

SMILES Code: C[C@@]12[C@](/C3=C\C(OC)=O)(OC(OC)(O3)C)CC[C@@]1([H])[C@]4([H])CCC5=CC(CC[C@]5([H])[C@@]4([H])CC2)=O

Appearance: White to off-white solid powder.

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: YK11 is a partial agonist of androgen receptor with osteogenic activity.
In vitro activity: A novel steroid compound, (17α,20E)-17,20-[(1-methoxyethylidene)bis(oxy)]-3-oxo-19-norpregna-4,20-diene-21-carboxylic acid methyl ester (YK11), was found to be a partial agonist of the androgen receptor (AR) in an androgen responsive element (ARE)luciferase reporter assay. YK11 accelerates nuclear translocation of AR. Furthermore, YK11 does not induce amino/carboxyl-terminal (N/C) interaction and prevents 5-α-dihydrotestosterone (DHT)-mediated N/C interaction. Thus, YK11 activates AR without causing N/C interaction, which may in turn be responsible for the partially agonistic nature of YK11 observed in the ARE-luciferase reporter system. YK11 acts as a gene-selective agonist of AR in MDA-MB 453 cells. The effect of YK11 on gene expression relative to that of androgen agonist varies depending on the gene context. YK11 activated the reporter gene by inducing the translocation of the AR into the nuclear compartment, where its amino-terminal domain (NTD) functions as a constitutive activator of AR target genes. These results suggest that YK11 might act as selective androgen receptor modulator (SARM). Reference: Biol Pharm Bull. 2011;34(3):318-23. https://pubmed.ncbi.nlm.nih.gov/21372378/
In vivo activity: The effect of YK11 on the pathophysiology of sepsis was tested. Sepsis was induced by i.p. injection of E. coli K1 at 1 × 108 CFU/mouse into mice that had a daily uptake of YK11 (6 h/3 times/day). YK11 injection at 350 and 700 mg/kg increased the survival rate of septic mice by 20% and 40%, respectively, within 72 h (Fig. 2A). YK11 also significantly reduced endotoxin levels in the serum (Fig. 2B), and the levels of inflammatory cytokines TNF-α, IL-1β, IL-6, IL-12p70, and IL-10 in the lungs of mice (Fig. 2C). Additionally, the levels of organ damage biomarkers—aspartate aminotransferase (AST), alanine aminotransferase (ALT) in the liver and blood urea nitrogen (BUN) in the kidneys—were alleviated by YK11 (Fig. 2D). Furthermore, YK11 promoted bacterial clearance from the organs of septic mice (Fig. 2E). It is YK11 effect was also shown against CRAB (Fig. S2). These data suggest that YK11 prevent septic mice caused by gram-negative bacteria by regulating inflammatory cytokine levels. Reference: Biochem Biophys Res Commun. 2021 Mar 5;543:1-7. https://pubmed.ncbi.nlm.nih.gov/33588136/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 64.0 148.65

Preparing Stock Solutions

The following data is based on the product molecular weight 430.541 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Lee SJ, Gharbi A, Shin JE, Jung ID, Park YM. Myostatin inhibitor YK11 as a preventative health supplement for bacterial sepsis. Biochem Biophys Res Commun. 2021 Mar 5;543:1-7. doi: 10.1016/j.bbrc.2021.01.030. Epub 2021 Feb 12. PMID: 33588136. 2. Piper T, Dib J, Putz M, Fusshöller G, Pop V, Lagojda A, Kuehne D, Geyer H, Schänzer W, Thevis M. Studies on the in vivo metabolism of the SARM YK11: Identification and characterization of metabolites potentially useful for doping controls. Drug Test Anal. 2018 Nov;10(11-12):1646-1656. doi: 10.1002/dta.2527. Epub 2018 Nov 18. PMID: 30379415. 3. Yatsu T, Kusakabe T, Kato K, Inouye Y, Nemoto K, Kanno Y. Selective Androgen Receptor Modulator, YK11, Up-Regulates Osteoblastic Proliferation and Differentiation in MC3T3-E1 Cells. Biol Pharm Bull. 2018;41(3):394-398. doi: 10.1248/bpb.b1700748. PMID: 29491216. 4. Kanno Y, Hikosaka R, Zhang SY, Inoue Y, Nakahama T, Kato K, Yamaguchi A, Tominaga N, Kohra S, Arizono K, Inouye Y. (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 receptor. Biol Pharm Bull. 2011;34(3):318-23. doi: 10.1248/bpb.34.318. PMID: 21372378.
In vitro protocol: 1. Yatsu T, Kusakabe T, Kato K, Inouye Y, Nemoto K, Kanno Y. Selective Androgen Receptor Modulator, YK11, Up-Regulates Osteoblastic Proliferation and Differentiation in MC3T3-E1 Cells. Biol Pharm Bull. 2018;41(3):394-398. doi: 10.1248/bpb.b1700748. PMID: 29491216. 2. Kanno Y, Hikosaka R, Zhang SY, Inoue Y, Nakahama T, Kato K, Yamaguchi A, Tominaga N, Kohra S, Arizono K, Inouye Y. (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 receptor. Biol Pharm Bull. 2011;34(3):318-23. doi: 10.1248/bpb.34.318. PMID: 21372378.
In vivo protocol: 1. Lee SJ, Gharbi A, Shin JE, Jung ID, Park YM. Myostatin inhibitor YK11 as a preventative health supplement for bacterial sepsis. Biochem Biophys Res Commun. 2021 Mar 5;543:1-7. doi: 10.1016/j.bbrc.2021.01.030. Epub 2021 Feb 12. PMID: 33588136. 2. Piper T, Dib J, Putz M, Fusshöller G, Pop V, Lagojda A, Kuehne D, Geyer H, Schänzer W, Thevis M. Studies on the in vivo metabolism of the SARM YK11: Identification and characterization of metabolites potentially useful for doping controls. Drug Test Anal. 2018 Nov;10(11-12):1646-1656. doi: 10.1002/dta.2527. Epub 2018 Nov 18. PMID: 30379415.

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1: Kanno Y, Ota R, Someya K, Kusakabe T, Kato K, Inouye Y. Selective androgen
receptor modulator, YK11, regulates myogenic differentiation of C2C12 myoblasts
by follistatin expression. Biol Pharm Bull. 2013;36(9):1460-5. PubMed PMID:
23995658.

2: Kanno Y, Hikosaka R, Zhang SY, Inoue Y, Nakahama T, Kato K, Yamaguchi A,
Tominaga N, Kohra S, Arizono K, Inouye Y.
(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
receptor. Biol Pharm Bull. 2011;34(3):318-23. PubMed PMID: 21372378.

YK11

25.0mg / USD 90.0