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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Neuronal Signal Pathway > BrexpiprazoleCAS：913611-97-9
Molecular Formula：C25H27N3O2S
Molecular Weight：433.57
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 913611-97-9 |
| Name | Brexpiprazole |
| Molecular Formula | C25H27N3O2S |
| Molecular Weight | 433.57 |
| Solubility | Soluble in DMSO ≥2mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 811-628-7 |
| MDL | MFCD27987920 |
| SMILES | O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1 |
| Target Point | 5-HT Receptor,Dopamine Receptor |
| Passage | Neuronal Signaling;GPCR & G Protein |
| Background | It is a novel partial agonist of dopamine receptor D2 and serotonin 1A receptor. |
| Biological Activity | Brexpiprazole (OPC-34712)是一种新型的多巴胺受体D2和5-羟色胺1A受体的部分激动剂，同时也是5-羟色胺2A受体和去甲肾上腺素alpha1B、alpha2C受体的拮抗剂。其对D2L, 5-HT1A, 5-HT2A, α1B受体和 α2C受体的Ki值分别为 0.3, 0.12, 0.47, 0.17 和 0.59 nM。[1] |
| IC50 | 5-HT1A(Cell-free assay):0.12nM(Ki);Dopamine D2L(Cell-free assay):0.3nM(Ki);5-HT2A receptors(Cell-free assay):0.47nM(Ki)[1] |
| In Vitro | Brexpiprazole是一种有效的人5-羟色胺 5-HT1A(Ki=0.12 nM)和多巴胺受体D2L(Ki=0.3 nM)的部分激活剂。还是5-HT2A受体的拮抗剂(Ki=0.47 nM)。它对人去甲肾上腺素受体α1B(Ki=0.17 nM)和α2C(Ki=0.59 nM)也有拮抗活性。此外，Brexpiprazole对人D3、5-HT2B、5-HT7、α1A和α1D肾上腺素能受体具有中等亲和力。在PC12细胞中，它能增强NGF引起的神经突增生、增强fluoxetine对神经突增生的作用[1]。 |
| In Vivo | Brexpiprazole在小鼠中通过5-HT1A受体，可改善由PCP-191引起的认知障碍[2]。 |
| Cell Experiment | 将细胞接种于细胞板后24小时，将培养基更换为DMEM培养基，包含0.5% FBS和1%青霉素-链霉素以及2.5 ng/ml神经生长因子，加入不同浓度的brexpiprazole(0，0.001，0.01，0.1 or 1.0 μM)。4天后，进行形态测定分析。[1] |
| Animal Experiment | Animal Models: ICR雄性小鼠; Dosages: 0.3，1或3 mg/kg/day; Administration: 口服[2] |
| Data Literature Source | [1] Ishima T，et al. Eur Neuropsychopharmacol. 2015，25(4):505-511. [2] Yoshimi N，et al. Pharmacol Biochem Behav. 2014，124:245-2 |
| Unit | Bottle |
| Specification | 5mg 10mg |
是一种新型的多巴胺受体D2和5-羟色胺1A受体的部分激动剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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