Asenapine Maleate

产品编号 T1951Cas号 85650-56-2

别名 Org 5222 maleate|||Org 5222|||马来酸阿塞那平|||阿塞那平马来酸盐

Asenapine Maleate (Org 5222 maleate) 是5-HT 和D2的拮抗剂，Ki 值分别为 0.03-4.0 nM, 1.3 nM。它也是抗精神病药物，用于治疗与双相 1 型障碍相关的精神分裂症和躁狂或混合发作。

Asenapine Maleate

产品编号 T1951别名 Org 5222 maleate, Org 5222, 马来酸阿塞那平, 阿塞那平马来酸盐Cas号 85650-56-2

规格	价格	库存
5 mg	¥ 229	现货
10 mg	¥ 372	现货
25 mg	¥ 631	现货
50 mg	¥ 970	现货
100 mg	¥ 1,730	现货
200 mg	¥ 2,990	现货
500 mg	¥ 4,830	现货
1 mL x 10 mM (in DMSO)	¥ 379	现货

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产品介绍

生物活性

产品描述	Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.
靶点活性	5-HT2A:10.15(pKi), 5-HT7:9.94(pKi), 5-HT6:9.6(pKi), 5-HT2B:9.75(pKi), 5-HT2C:10.46(pKi)
体外活性	Asenapine（0.01 mg/kg,i.v.）与NAc核相比,壳内优先增加多巴胺的流出量,而高剂量(0.05 mg/kg, i.v.)则无差异.在内侧前额叶皮质的锥体细胞中,Asenapine对NMDA诱导的应答有显著增强作用.在自由移动的大鼠中,Asenapine（0.05-0.2 mg/kg,皮下注射）诱导剂量依赖性CAR抑制（无逃避失败记录）,且未诱发强直性昏厥.在大鼠在内侧前额叶皮质和伏隔核中,Asenapine（0.05-0.2 mg/kg,皮下注射）同时增加多巴胺流出.
体内活性	相对于其D2受体亲和力,Asenapine对5-HT 2C,5-HT 2A,5-HT 2B,5-HT 7,5-HT 6,alpha2B和D3受体的亲和力更高,说明在治疗剂量下其与这些靶标联系更紧密。Asenapine是一种对5-HT 1A（7.4）,5-HT1B（8.1）,5-HT 2A（9.0）,5-HT 2B（9.3）,5-HT 2C（9.0）,5-HT 6（8.0 ）,5-HT 7（8.5）,D2（9.1）,D3（9.1）,alpha2A（7.3）,alpha2B（8.3）,alpha2C（6.8）和H 1受体（8.4）有效的拮抗剂（pKB）。
激酶实验	In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service.
别名	Org 5222 maleate, Org 5222, 马来酸阿塞那平, 阿塞那平马来酸盐

化学信息

分子量	401.84
分子式	C₂₁H₂₀ClNO₅
CAS No.	85650-56-2

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 60 mg/mL (149.31 mM), Sonication is recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4886 mL	12.4428 mL	24.8855 mL	124.4276 mL
5 mM	0.4977 mL	2.4886 mL	4.9771 mL	24.8855 mL
10 mM	0.2489 mL	1.2443 mL	2.4886 mL	12.4428 mL
20 mM	0.1244 mL	0.6221 mL	1.2443 mL	6.2214 mL
50 mM	0.0498 mL	0.2489 mL	0.4977 mL	2.4886 mL
100 mM	0.0249 mL	0.1244 mL	0.2489 mL	1.2443 mL