CL 218872

Name: CL 218872
Brand: TargetMol
SKU: T8572
Price: 121 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.92%

货号 T8572Cas号 66548-69-4

CL218872 是口服有活性的苯二氮卓类选择性激动剂，激动含有 α1 亚基的GABAA 受体(Ki:130 nM)。它在体内具有抗惊厥及抗焦虑效果。

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CL 218872

一键复制产品信息

很棒

纯度: 99.92%

货号 T8572Cas号 66548-69-4

CL218872 是口服有活性的苯二氮卓类选择性激动剂，激动含有 α1 亚基的GABAA 受体(Ki:130 nM)。它在体内具有抗惊厥及抗焦虑效果。

规格	价格	库存
5 mg	¥ 121	现货
10 mg	¥ 173	现货
25 mg	¥ 366	现货
50 mg	¥ 608	现货
100 mg	¥ 861	现货
200 mg	¥ 1,280	现货
1 mL x 10 mM (in DMSO)	¥ 125	现货

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纯度: 99.92%

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COA HNMR LCMS 产品操作手册

产品介绍

CL 218872 AI Summary

CL 218872 exhibits significant bioactivity across various systems, predominantly influencing GABAergic neurotransmission. It demonstrates binding affinities with multiple subunits of the GABA-A receptor, showing strong affinity particularly for the alpha-1-beta-3-gamma-2 subunits (Ki = 57.0 nM) and moderate affinities for other subunits such as alpha-3-beta-3-gamma-2 (Ki = 1161.0 nM) and alpha-5-beta-3-gamma-2 (Ki = 561.0 nM). It binds to various GABA-A receptor subtypes with Ki values ranging from 57.0 nM to greater than 10000.0 nM, indicating selective bioactivity towards certain subtypes. Additionally, CL 218872 exhibits anticonvulsant activity, demonstrated by its efficacy in preventing convulsions in mice, and shows anxiolytic properties by protecting against pentylenetetrazole-induced convulsions. Moreover, CL 218872 shows binding affinity for the benzodiazepine receptor (Ki = 198.0 nM) and relative binding to the central benzodiazepine receptor with a GABA ratio of 1.2 in the presence and absence of 10e-4 M GABA. This suggests potential modulation of GABAergic neurotransmission through interaction with benzodiazepine sites. In addition to its neurological activities, CL 218872 has shown inhibitory effects on various targets, including enzymes like Cytochrome P450 3A4, ALDH1A1, and HPGD, and it exhibits antiviral activity against SARS-CoV-2, providing broad pharmacological potential. It inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells and demonstrates modest inhibition of SARS-CoV-2 3CL-Pro protease. Overall, CL 218872 is a potent GABA-A receptor modulator with anticonvulsant and anxiolytic properties, alongside exhibiting significant enzymatic and antiviral bioactivities..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 nM for α1, α2, α3, α4, α5 and α6-subunit containing receptors respectively). Orally active anxiolytic and anticonvulsant in vivo.

化学信息

分子量	278.23
分子式	C₁₃H₉F₃N₄
CAS No.	66548-69-4
Smiles	CC=1N2C(C=CC(=N2)C3=CC(C(F)(F)F)=CC=C3)=NN1
密度	1.43g/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

DMSO: 13.9 mg/mL (49.96 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.5941 mL	17.9707 mL	35.9415 mL	179.7074 mL
5 mM	0.7188 mL	3.5941 mL	7.1883 mL	35.9415 mL
10 mM	0.3594 mL	1.7971 mL	3.5941 mL	17.9707 mL
20 mM	0.1797 mL	0.8985 mL	1.7971 mL	8.9854 mL