Felcisetrag (TAK-954, TD-8954)

Chemical Structure : Felcisetrag

CAS No.: 916075-84-8

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货号: PC-73307Not For Human Use, Lab Use Only.

Felcisetrag (TAK-954, TD-8954) is a highly selective and potent 5-HT4 receptor agonist with pKi of 9.4 (human 5-HT4).

规格	价格	库存
5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Felcisetrag (TAK-954, TD-8954) is a highly selective and potent 5-HT4 receptor agonist with pKi of 9.4 (human 5-HT4).
Felcisetrag (TAK-954, TD-8954) displays high selectivity (>2,000-fold) over all other 5-HT receptors and non-5-HT receptors, ion channels, enzymes and transporters.
Felcisetrag (TAK-954, TD-8954) produced an elevation of cAMP in HEK-293 cells expressing the h5-HT(4(c)) receptor (pEC=9.3), and contracted the guinea pig colonic longitudinal muscle/myenteric plexus preparation (pEC50=8.6).
Felcisetrag (TAK-954, TD-8954) (0.03-3 mg/kg) increased the colonic transit of carmine red dye, reducing the time taken for its excretion.
Felcisetrag (TAK-954, TD-8954) demonstrated robust in vivo stimulatory activity in the gastrointestinal (GI) tract of guinea pigs, rats, dogs, and humans.

物理化学性质&存储条件

分子量	455.603
分子式	C25H37N5O3
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	methyl 4-[[4-[[(2-propan-2-yl-1H-benzimidazole-4-carbonyl)amino]methyl]piperidin-1-yl]methyl]piperidine-1-carboxylate

参考文献

1. Shen F, et al. Neuropharmacology. 2011 Jul-Aug;61(1-2):69-79.

2. Beattie DT, et al. Front Pharmacol. 2011 May 30;2:25.

3. Beattie DT, et al. Vascul Pharmacol. 2013 Jan;58(1-2):150-6.