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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-ABT-594 dihydrochloride
ABT-594 dihydrochloride

Chemical Structure : ABT-594 dihydrochloride

CAS No.: 209326-19-2

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ABT-594 dihydrochloride (Tebanicline dihydrochloride)

货号: PC-21602Not For Human Use, Lab Use Only.

Tebanicline dihydrochloride (ABT-594) is a potent, orally active neuronal nicotinic acetylcholine receptor (alpha 4 beta 2 nAChR) agonist with Ki of 37 pM (rat brain) and 55 pM (transfected human receptor).

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3280 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tebanicline dihydrochloride (ABT-594) is a potent, orally active neuronal nicotinic acetylcholine receptor (alpha 4 beta 2 nAChR) agonist with Ki of 37 pM (rat brain) and 55 pM (transfected human receptor).
Tebanicline dihydrochloride (ABT-594) is 180,000-fold selectivity for the neuronal alpha 4 beta 2 nAChR over alpha 1 beta 1 delta gamma neuromuscular nAChR.
Tebanicline dihydrochloride (ABT-594) has weak affinity in binding assays for adrenoreceptor subtypes alpha-1B (Ki = 890 nM), alpha-2B (Ki=597 nM) and alpha-2C (Ki=342 nM), and it has negligible affinity (Ki > 1000 nM) for approximately 70 other receptors, enzyme and transporter binding sites.
Tebanicline dihydrochloride (ABT-594) has an EC50 value of 140 nM with an intrinsic activity in human alpha 4 beta 2 neuronal nAChR (K177 cells).
Tebanicline dihydrochloride (ABT-594) (30 uM) inhibits the release of calcitonin gene-related peptide from C-fibers terminating in the dorsal horn of the spinal cord, an effect mediated via nAChRs.

物理化学性质&存储条件

分子量 271.57
分子式 C9H13Cl3N2O
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

Pyridine, 5-[(2R)-2-azetidinylmethoxy]-2-chloro-, hydrochloride (1:2)

参考文献

1. Bannon AW, et al. J Pharmacol Exp Ther. 1998 May;285(2):787-94.

2. Holladay MW, et al. J Med Chem. 1998 Feb 12;41(4):407-12.

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