产品名称

英文名称：MK-0773

同义词

MK-0773、606101-58-0、PF-05314882、CHEMBL3221237、5730VNW22X、(1S,3aS,3bS,5aR,9aS,9bS,11aS)-8-fluoro-N-(1H-imidazo[4,5-b]pyridin-2-ylmethyl)-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,9b,10,11-decahydro-1H-indeno[5,4-f]quinoline-1-carboxamide、(4aS,4bS,6aS,7S,9a

产品性质

CAS编号：606101-58-0

分子式：C27H34FN5O2

分子量：479.59

PubChem编号：11950726

英文别名：MK-0773|606101-58-0|PF-05314882|CHEMBL3221237|5730VNW22X|(1S,3aS,3bS,5aR,9aS,9bS,11aS)-8-fluoro-N-(1H-imidazo[4,5-b]pyridin-2-ylmethyl)-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,9b,10,11-decahydro-1H-indeno[5,4-f]quinoline-1-carboxamide|(4aS,4bS,6aS,7S,9a

规格或纯度：≥99%

英文名称：MK-0773

生化机理：DescriptionIC50 Value 6.6 nM [1]MK-0773, one of Selective androgen receptor modulators (SARMs), is a 4-aza-steroid that exhibited tissue selectivity in humans.in vitro The IC50 of MK-0773 binding to AR was increased 3.5-fold in the presence of 25% rat serum and 13-fold in the presence of 25% human serum, indicating that it binds to serum proteins. 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) [1].in vivo MK-0773 was dosed subcutaneously for 24 days in the OVX rat model (6 and 80 mg/kg) and produced plasma exposures over 24 h of 6.6 and 62 μM·h. This treatment produced exposure-related stimulatory effects on cortical BFR and LBM. The maximal anabolic effects of MK-0773 were equivalent to the SARM TFM-4AS-1 and ?80% of 3 mg/kg DHT [1]. Participants receiving MK-0773 showed a statistically significant increase in LBM from baseline at Month 6 vs. placebo (p<0.001). Participants receiving both MK-0773 and placebo showed a statistically significant increase in strength from baseline to Month 6, but the mean difference between the two groups was not significant (p=0.269) [2].Clinical trial Safety, Tolerability and Efficacy of MK-0773 in Healthy Postmenopausal Women. Phase 1

储存温度：-20°C储存

运输条件：超低温冰袋运输

IUPAC Name：(1S,3aS,3bS,5aR,9aS,9bS,11aS)-8-fluoro-N-(1H-imidazo[4,5-b]pyridin-2-ylmethyl)-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,9b,10,11-decahydro-1H-indeno[5,4-f]quinoline-1-carboxamide

INCHI：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

InChi Key：GBEUKTWTUSPHEE-JWJWXJQQSA-N

Canonical SMILES：CC12CCC3C(C1CCC2C(=O)NCC4=NC5=C(N4)C=CC=N5)CCC6C3(C=C(C(=O)N6C)F)C

Isomeric SMILES：C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2C(=O)NCC4=NC5=C(N4)C=CC=N5)CC[C@@H]6[C@@]3(C=C(C(=O)N6C)F)C

PubChem CID：11950726

溶解性：25°C DMSO

产品包装