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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-Cebranopadol
Cebranopadol

Chemical Structure : Cebranopadol

CAS No.: 863513-91-1

Cebranopadol (GRT-6005;GRT 6005;GRT6005)

货号: PC-35217Not For Human Use, Lab Use Only.

Cebranopadol (GRT-6005, GRT6005) is a potent analgesic nociceptin/orphanin FQ peptide (NOP receptor, ORL1) and opioid receptor agonist with Ki/EC50 of 0.9/13 nM (human NOP receptor), 0.7/1.2 nM (mu-opioid receptor).

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10 mg ¥2180 In stock
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50 mg ¥5980 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

Cebranopadol (GRT-6005, GRT6005) is a potent analgesic nociceptin/orphanin FQ peptide (NOP receptor, ORL1) and opioid receptor agonist with Ki/EC50 of 0.9/13 nM (human NOP receptor), 0.7/1.2 nM (mu-opioid receptor).
Cebranopadol exhibits highly potent and efficacious antinociceptive and antihypersensitive effects in several rat models of acute and chronic pain with ED50 values of 0.5-5.6 µg/kg after oral administration, does not disrupt motor coordination and respiration.

物理化学性质&存储条件

分子量 378.491
分子式 C24H27FN2O
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

(1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1'-pyrano[3,4-b]indol]-4-amine

参考文献

1. Linz K, et al. J Pharmacol Exp Ther. 2014 Jun;349(3):535-48.

2. Schunk S, et al. ACS Med Chem Lett. 2014 Jun 24;5(8):857-62.

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