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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-RS-102221
RS-102221

Chemical Structure : RS-102221

CAS No.: 187397-18-8

RS-102221 (RS102221)

货号: PC-60815Not For Human Use, Lab Use Only.

RS-102221 is a highly potent, selective 5-HT2C receptor antagonist with pKi of 8.4 and 8.5 for human and rat 5-HT2C, respectively.

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 ¥5280 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

RS-102221 is a highly potent, selective 5-HT2C receptor antagonist with pKi of 8.4 and 8.5 for human and rat 5-HT2C, respectively.
RS-102221 demonstrates 100-fold selectivity for the 5-HT2C versus 5-HT2A and 5-HT2B receptors.
RS-102221 acts as an antagonist in a cell-based microphysiometry functional assay with pA2 of 8.1 and has no detectable intrinsic efficacy; increases food-intake and weight-gain in rats (2 mg/kg, i.p.).
RS-102221 reverses the inhibitory effects of MK-212 and DOI on 'monosynaptic and 'intermediate' neurones.

物理化学性质&存储条件

分子量 649.08
分子式 C27H31F3N4O7S.HCl
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

8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl-5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione hydrochloride

参考文献

1. Bonhaus DW, et al. Neuropharmacology. 1997 Apr-May;36(4-5):621-9.

2. Bonhaus DW, et al. Ann N Y Acad Sci. 1998 Dec 15;861:269.

3. Sévoz-Couche C, et al. Br J Pharmacol. 2000 Dec;131(7):1445-53.

4. McMahon LR, et al. J Neurosci. 2001 Oct 1;21(19):7781-7.

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