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Amisulpride

Name: Amisulpride
Brand: TargetMol
SKU: T0811
Price: 116 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.99%

货号 T0811Cas号 71675-85-9

别名 氨磺必利, 阿米舒必利, DAN 2163

Amisulpride (DAN 2163) 是多巴胺D2/D3受体拮抗剂，对于人多巴胺D2和D3的Ki 分别为 2.8 和 3.2 nM。

Amisulpride

一键复制产品信息

很棒

纯度: 99.99%

货号 T0811 别名 氨磺必利, 阿米舒必利, DAN 2163Cas号 71675-85-9

Amisulpride (DAN 2163) 是多巴胺D2/D3受体拮抗剂，对于人多巴胺D2和D3的Ki 分别为 2.8 和 3.2 nM。

规格	价格	库存
2 mg	¥ 116	现货
5 mg	¥ 169	现货
10 mg	¥ 236	现货
25 mg	¥ 375	现货
50 mg	¥ 543	现货
100 mg	¥ 795	现货
500 mg	¥ 1,990	现货
1 mL x 10 mM (in DMSO)	¥ 239	现货

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产品介绍

Amisulpride AI Summary

Amisulpride exhibits a diverse range of bioactivities, including significant interactions with various human receptors and enzymes. It has high affinity for the human dopamine D2 (Ki = 12.59 nM) and D3 receptors (Ki = 3.981 nM), as well as the 5HT2B (Ki = 316.23 nM), 5HT2A (Ki = 630.96 nM), and 5HT7 receptors (Ki = 25.12 nM). The compound also shows affinity for the adrenergic alpha-2 receptor in rat cerebral cortex (Ki = 125.89 nM). Additionally, it exhibits potent antagonistic activity at the D2 receptor in CHOK1 cells co-expressing G-alpha 15, with an IC50 of 3.04 nM. In terms of pharmacokinetics, Amisulpride demonstrates good bioavailability (fraction absorbed, Fa = 1.0) and a high fraction unbound in human plasma (Fu = 0.84). Its total body clearance (CL) is 7.8 mL.min-1.kg-1, with renal clearance (CL_renal) of 4.4 mL.min-1.kg-1 and a moderate volume of distribution at steady state (Vdss = 5.8 L.kg-1). The compound is highly soluble in 0.1 M phosphate buffer (600 µM at pH 7.4) and exhibits a strong solubility exceeding 500,000 nM. Amisulpride has been identified to inhibit several enzymes and pathways, including Bacillus subtilis Sfp phosphopantetheinyl transferase, human lipoxygenase (15-hLO), Histone Lysine Methyltransferase G9a, ERK signaling, and Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1). Furthermore, it shows antiviral activity against SARS-CoV-2, inhibiting virus-induced cytotoxicity and the 3CL-Pro protease, as well as demonstrating effects on VERO-6 and HRCE cells. In antimicrobial assays, Amisulpride displays inhibitory activity against several bacterial and fungal pathogens, including moderate inhibition of Pseudomonas aeruginosa and Staphylococcus aureus MRSA, and antifungal activity against Candida albicans. The compound shows minimal hepatotoxicity with low incidences of liver toxicity and specific bioactivity against transport proteins such as BSEP, MRP2, MRP3, and MRP4. It further exhibits inhibitory activity against human HDAC6 and SET7, as measured by enzymatic assays. Overall, Amisulpride's broad spectrum of bioactivities and favorable pharmacokinetic properties suggest its potential utility in diverse therapeutic applications..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Amisulpride (DAN 2163) (trade name Solian) is an antipsychotic drug sold by Sanofi-Aventis. It is not approved for use in the United States, but is approved for use in Europe and Australia for the treatment of psychoses and schizophrenia. Additionally, it is approved in Italy for the treatment of dysthymia (under the brand name Deniban). Amisulpride is a selective dopamine antagonist.
靶点活性	D3 receptor:3.2 nM (Ki), D2 receptor:2.8 nM (Ki)
别名	氨磺必利, 阿米舒必利, DAN 2163

化学信息

分子量	369.48
分子式	C₁₇H₂₇N₃O₄S
CAS No.	71675-85-9
Smiles	C(NCC1N(CC)CCC1)(=O)C2=C(OC)C=C(N)C(S(CC)(=O)=O)=C2
密度	1.2 g/cm3
颜色	White
物理性状	Solid

储存&溶解度

存储

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

溶解度信息

Ethanol: 65 mg/mL (175.92 mM), Sonication is recommended.

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

DMSO: 50 mg/mL (135.33 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.41 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.7065 mL	13.5325 mL	27.0651 mL	135.3253 mL
5 mM	0.5413 mL	2.7065 mL	5.4130 mL	27.0651 mL
10 mM	0.2707 mL	1.3533 mL	2.7065 mL	13.5325 mL
20 mM	0.1353 mL	0.6766 mL	1.3533 mL	6.7663 mL
50 mM	0.0541 mL	0.2707 mL	0.5413 mL	2.7065 mL
100 mM	0.0271 mL	0.1353 mL	0.2707 mL	1.3533 mL