MK-0773

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C27H34FN5O2
Molecular Weight	479.5896
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12CC[C@H](C(=O)NCC3=NC4=C(N3)C=CC=N4)[C@@]1(C)CC[C@@]5([H])[C@@]2([H])CC[C@@]6([H])N(C)C(=O)C(F)=C[C@]56C

InChI

InChIKey=GBEUKTWTUSPHEE-JWJWXJQQSA-N

InChI=1S/C27H34FN5O2/c1-26-11-10-17-15(6-9-21-27(17,2)13-19(28)25(35)33(21)3)16(26)7-8-18(26)24(34)30-14-22-31-20-5-4-12-29-23(20)32-22/h4-5,12-13,15-18,21H,6-11,14H2,1-3H3,(H,30,34)(H,29,31,32)/t15-,16-,17-,18+,21+,26-,27+/m0/s1

HIDE SMILES / InChI

Molecular Formula	C27H34FN5O2
Molecular Weight	479.5896
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	7 / 7
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23732550 | https://www.ncbi.nlm.nih.gov/pubmed/24189892 | https://www.pharmacodia.com/yaodu/html/v1/chemicals/94b7cee526e7478a1d4c97340d74b467.html

MK-0773 is an orally active selective androgen receptor modulator. The safety and efficacy of MK-0773 was evaluated in sarcopenic elderly women. The MK-0773- induced improvements in lean body mass were not accompanied by statistically significant improvements in physical function. Higher dose of MK-0773 or longer duration of therapy might have resulted in improvements in physical function, but liver transaminase elevations likely preclude further development of MK-0773. Drug-candidate had been in phase I clinical trials for the treatment of osteoporosis.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Androgen Receptor 167 Target ID: CHEMBL1871 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20356837	Partial Agonist 290		6.6 nM [IC50]
HERG 92 Target ID: CHEMBL240 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20356837	Binding Agent 1064		49.5 µM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Sarcopenia 3 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23732550	Primary		Phase II 1132	Unknown Approved Use Unknown
Osteoporosis 97 Sources: https://clinicaltrials.gov/ct2/show/NCT01011725	Primary		Phase I 428	Unknown Approved Use Unknown

Sourcing

Vendor/Aggregator	ID	URL
AbovChem LLC	HY-11027
BLD Pharm	BD630789	http://www.bldpharm.com/search/Search.html?keyword=BD630789
Chem Scene	CS-1508	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-1508
MedChem Express	HY-11027	https://www.medchemexpress.com/search.html?q=HY-11027&ft=&fa=&fp=
MolPort	MolPort-046-416-876	https://www.molport.com/shop/molecule-link/MolPort-046-416-876
Molnova	M15267	https://www.molnova.com/en/serch-list.html?keywords=M15267
Toronto Research Chemicals	M424980	https://www.trc-canada.com/product-detail/?CatNum=M424980
eMolecules	50283015	https://orderbb.emolecules.com/search/#?query=50283015
mcule	MCULE-6964976801	https://mcule.com/MCULE-6964976801/

PubMed

Title	Date	PubMed
Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer.	2013 Dec	24189892
Identification of selected in vitro generated phase-I metabolites of the steroidal selective androgen receptor modulator MK-0773 for doping control purposes.	2016	27419898
Detection of SARMs in doping control analysis.	2018 Mar 15	28137616

Patents

Sample Use Guides

In Vivo Use Guide

50 mg twice daily, 6 month treatment period

Route of Administration: Oral

In Vitro Use Guide

The affinity of MK-0773 for AR across species was evaluated using COS cells transfected with AR, and IC50 values were very similar in four species (rat, 0.50 nM; dog, 0.55 nM; rhesus, 0.45 nM; human, 0.65 nM).

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:49:53 UTC 2023` Edited by `admin` on `Fri Dec 15 16:49:53 UTC 2023`
Record UNII	5730VNW22X
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MK-0773

Common Name

English

PF-05314882

Code

English

N-(3H-IMIDAZO(4,5-B)PYRIDIN-2-YLMETHYL)-2-FLUORO-4-METHYL-3-OXO-4-AZA-5.ALPHA.-ANDROST-1-ENE-17.BETA.-CARBOXAMIDE

Systematic Name

English

Code System Code Type Description

ChEMBL

CHEMBL3545333