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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-SB 242084 hydrochloride
SB 242084 hydrochloride

Chemical Structure : SB 242084 hydrochloride

CAS No.: 1049747-87-6

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SB 242084 hydrochloride (SB242084 hydrochloride)

货号: PC-43516Not For Human Use, Lab Use Only.

SB 242084 hydrochloride is a potent, selective, brain penetrant 5-HT2C receptor antagonist with pKi of 9.0, 100- and 158-fold selectivity over the closely related 5-HT2B and 5-HT2A subtypes.

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10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2680 In stock
100 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

SB 242084 hydrochloride is a potent, selective, brain penetrant 5-HT2C receptor antagonist with pKi of 9.0, 100- and 158-fold selectivity over the closely related 5-HT2B and 5-HT2A subtypes.
SB 242084 hydrochloride also displays >100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors.
SB 242084 hydrochloride inhibits 5-HT-stimulated phosphatidylinositol hydrolysis with pKb of 9.3 in cell-baed assays.
SB 242084 hydrochloride potently inhibits m-chlorophenylpiperazine (mCPP)-induced hypolocomotion in rats, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o.

物理化学性质&存储条件

分子量 467.78
分子式 C21H21Cl3N4O2
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

1H-Indole-1-carboxamide, 6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-, hydrochloride (1:2)

参考文献

1. Bromidge SM, et al. J Med Chem. 1997 Oct 24;40(22):3494-6.

2. Kennett GA, et al. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.

3. Di Matteo V, et al. Neuropharmacology. 1999 Aug;38(8):1195-205.

4. Higgins GA, et al. Br J Pharmacol. 2001 Jun;133(4):459-66.

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