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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-SAGE-718
SAGE-718

Chemical Structure : SAGE-718

CAS No.: 1629853-48-0

SAGE-718 (Dalzanemdor, SAGE718)

货号: PC-49063Not For Human Use, Lab Use Only.

Dalzanemdor (SAGE-718) is a potent and high intrinsic activity N-Methyl-d-aspartate receptor (NMDAR) positive allosteric modulator with EC50 of 86 and 79 nM for GluN2A and GluN2B, respectively, reverses DOI-induced increases in locomotor activity.

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5 mg ¥9880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Dalzanemdor (SAGE-718) is a potent and high intrinsic activity N-Methyl-d-aspartate receptor (NMDAR) positive allosteric modulator with EC50 of 86 and 79 nM for GluN2A and GluN2B, respectively, reverses DOI-induced increases in locomotor activity.
Administration of SAGE-718 (1 mg/kg DOI) significantly increased locomotor activity and rearing compared to vehicle.
Acute administration of SAGE-718 (5-10 mg/kg) significantly reduced DOI-induced increases in distance traveled and rearing during the first 30 min after DOI administration.
SAGE-718 is currently in a placebo-controlled phase 2 clinical study to evaluate its impact on cognitive deficits in an HD patient population.

物理化学性质&存储条件

分子量 456.634
分子式 C27H43F3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(3S,8S,9S,10R,13R,14S,17R)-3,10,13-Trimethyl-17-((2R,5S)-6,6,6-trifluoro-5-hydroxy-5-methylhexan-2-yl)-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-ol

参考文献

1. Matthew D Hill, et al. J Med Chem. 2022 Jul 2. doi: 10.1021/acs.jmedchem.2c00313.

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