SB-277011 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB-277011 hydrochloride (SB-277011A hydrochloride) 是一种强效、选择性、口服生物利用度和脑透多巴胺 D3 受体(D3R) 拮抗剂，其 Ki 值在啮齿动物和人D3R 分别为 10.7 nM 和 11.2 nM。SB-277011 hydrochloride 对 D3 受体比其他多巴胺受体表现出 80-100 倍的选择性，，对 D3，D2，5-HT1B?和 5-HT1D 受体的?pKi 值分别为 8.0，6.0，<5.2 和 5.9。

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate?dopamine D3?receptor (D3R)?antagonist with Ki values of 10.7?nM and?11.2 nM?at?rodent and human?D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with?pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.

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SB-277011 hydrochloride has an excellent pharmacokinetic profile, exhibits oral bioavailability 43%, half-life:2.0 h, plasma clearance 19 mL/min/kg) and to be highly brain-penetrant (brain:blood ratio of 3.6:1), with a clean P450 profile in the rat.SB-277011 hydrochloride (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats.SB-277011 (intraperitoneal injection; 12.5-25 mg/kg) significantly and dose-dependently reduces intravenous cocaine self-administration under both low fixed-ratio and progressive-ratio reinforcement conditions in rats. When it increases to 50 mg/kg, SB-277011 can significantly inhibit basal and cocaine-enhanced locomotion in rats.

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GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

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215804-67-4

475.03

C28H31ClN4O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (105.26 mM; 超声助溶 ) H2O 中的溶解度 : 16.67 mg/mL (35.09 mM; 超声助溶)

C(N[C@@H]1CC[C@@H](CCN2CC=3C(CC2)=CC(C#N)=CC3)CC1)(=O)C=4C5=C(N=CC4)C=CC=C5.Cl

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(-20℃)

With Ice Pack

≥ 2 years