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S80077

Cariprazine (hydrochloride)

源叶(MedMol) 99%
  • 英文名:
  • Cariprazine (hydrochloride)
  • 别名:
  • Cariprazine hydrochloride; Cariprazine hydrochloride [USAN]; RGH-188 HCL; Cariprazine HCl; UNII-KQD7C255YG; trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexyla
  • CAS号:
  • 1083076-69-0
  • 分子式:
  • C21H33Cl3N4O
  • 分子量:
  • 463.8719
  • 核磁/质谱:
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源叶(MedMol) S80077-5mg 99% ¥235.00元 10 - - - EA 加入购物车
源叶(MedMol) S80077-10mg 99% ¥385.00元 >10 - - - EA 加入购物车
源叶(MedMol) S80077-50mg 99% ¥970.00元 7 - - - EA 加入购物车
源叶(MedMol) S80077-100mg 99% ¥1470.00元 5 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Cariprazine hydrochloride is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
  • 靶点: D2 Receptor:0.49 nM (Ki);D3 Receptor:0.085 nM (Ki);5-HT1A Receptor:2.6 nM (Ki);DopamineReceptor;5-HTReceptor
  • 体外研究:
    Cariprazine stimulates inositol phosphate (IP) formation with a high potency (pEC50 8.5) with relatively low efficacy (Emax 30%). Cariprazine, a novel candidate antipsychotic, demonstrated approximately 10-fold higher affinity for human D3 versus human D2L and human D2S receptors (pKi 10.07, 9.16, and 9.31, respectively). Cariprazine displays high affinity at human serotonin (5-HT) type 2B receptors (pKi 9.24) with pure antagonism. Cariprazine has lower affinity at human and rat hippocampal 5-HT1A receptors (pKi 8.59 and 8.34, respectively) and demonstrates low intrinsic efficacy. Cariprazine displays low affinity at human 5-HT2A receptors (pKi 7.73). Moderate or low affinity for histamine H1 and 5-HT2C receptors (pKi 7.63 and 6.87, respectively) suggest Cariprazine's reduced propensity for adverse events related to these receptors. Cariprazine is over sixfold more potent (EC50=1.4 nM) than Aripiprazole (EC50=9.2 nM) in inhibiting isoproterenol-induced cAMP production in HEK-293 cells
  • 体内研究:
    Administration of Cariprazine (30 µg/kg) reduces the striatal uptake of both radioligands to the level of nonspecific binding compared with baseline PET measurements. Cariprazine has negligible effect on the time-activity curves in the cerebellum. At doses of 5.0 and 30 µg/kg, Cariprazine causes a dose-dependent dopamine D2/D3 receptor occupancy of ~45% and ~80% for both antagonist [11C] raclopride and agonist radioligand [11C]MNPA. Receptor occupancy of dopamine D2/D3 receptors calculated using the transient equilibrium and the MRTM2 methods ranged from 5% at the lowest dose (1.0 µg/kg) to 94% at the highest dose (300 µg/kg). The effects of 5 doses of Cariprazine (ranging from 0.005 to 0.15 mg/kg) are examined on EPM behavior of wild-type mice. Whereas lower doses of Cariprazine (0.005 to 0.02 mg/kg) do not alter the time spent in open arms, the two higher doses (0.08 and 0.15 mg/kg) lead to a significant decline of this measure (ANOVA, (F(5,52)=4.20; p=0.0032)). Moreover, the two higher doses of Cariprazine also lead to a significant decrease in the total number of arm entries (F(5,52)=7.21; p=0.0001)) but this decrease in the total number of arm entries is largely accounted for by a significant decrease in the number of closed arm entries (F(5,52)=11.75; p=0.0001)). The two highest doses of Cariprazine (0.08 and 0.15 mg/kg) have significant effects on locomotor activity, but doses ranging from 0.005 to 0.02 mg/kg do not affect anxiety-like behavior or locomotor activity in the EPM test. A signifi
  • 参考文献:
    1. Seneca N, et al. Occupancy of dopamine D2 and D3 and serotonin 5-HT1A receptors by the novel antipsychotic drug candidate, cariprazine (RGH-188), in monkey brain measured using positron emission tomography. Psychopharmacology (Berl). 2011 Dec;218(3):579-8 2. Kiss B, et al. Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile. J Pharmacol Exp Ther. 2010 Apr;333(1):328-40. 3. Zimnisky R, et al. Cariprazine, a dopamine D(3)-receptor-preferring partial agonist, blocks phencyclidine-induced impairments of working memory, attention set-shifting, and recognition memory in the mouse. Psychopharmacology (Berl). 2013 Mar;226(1):91-100. 4. Gao Y, et al. Cariprazine exerts antimanic properties and interferes with dopamine D2 receptor β-arrestin interactions. Pharmacol Res Perspect. 2015 Feb;3(1):e00073. 5. Citrome L. Cariprazine in schizophrenia: clinical efficacy, tolerability, and place in therapy. Adv Ther. 2013 Feb;30(2):114-26.
  • 溶解性: Soluble  in  DMSO、H2O
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.156 ml 10.779 ml 21.558 ml
    5 mM 0.431 ml 2.156 ml 4.312 ml
    10 mM 0.216 ml 1.078 ml 2.156 ml
    50 mM 0.043 ml 0.216 ml 0.431 ml
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