SB 277011A dihydrochloride

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CAS NO:

1226917-67-4

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

SB 277011A dihydrochloride (SB-277011A dihydrochloride) 是一种有效的、选择性的、口服生物利用度和脑穿透多巴胺 D3 受体拮抗剂，对 D3、D2、5-HT1B 和 5-HT1D 受体的 pKis 分别为 8.0、6.0、<5.2 和 5.9 ，分别。

Cas No.	1226917-67-4
别名	SB-277011A dihydrochloride
化学名	N-((1r,4r)-4-(2-(6-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)quinoline-4-carboxamide dihydrochloride
Canonical SMILES	N#CC1=CC(CCN2CC[C@@]3([H])CC[C@@](NC(C4=CC=NC5=CC=CC=C45)=O)([H])CC3)=C(C2)C=C1.Cl.Cl
分子式	C₂₈H₃₀N₄O.2HCl
分子量	511.49
溶解度	DMF: 3 mg/ml,DMSO: 14 mg/ml,DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml,Ethanol: 0.1 mg/ml
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0,<5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively. SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, and restores ≥100-fold selectivity against the D2, 5-HT1B, and 5-HT1D receptors, with pKis of 8.0, 6.0,<5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1]. SB-277011 dihydrochloride (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[1]. References: [1]. Stemp G, et al. Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. J Med Chem. 2000 May 4;43(9):1878-85.