Org 25543

Name: Org 25543
Brand: TargetMol
SKU: T50082
Price: 475 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.13%

货号 T50082Cas号 363628-88-0

Org 25543 是一种 N-酰基氨基酸的开发，它选择性地抑制甘氨酸转运蛋白 2 以在大鼠慢性疼痛模型中产生镇痛作用。

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Org 25543

一键复制产品信息

很棒

纯度: 99.13%

货号 T50082Cas号 363628-88-0

Org 25543 是一种 N-酰基氨基酸的开发，它选择性地抑制甘氨酸转运蛋白 2 以在大鼠慢性疼痛模型中产生镇痛作用。

规格	价格	库存
1 mg	¥ 475	现货
5 mg	¥ 1,090	现货
10 mg	¥ 1,630	现货
25 mg	¥ 2,650	现货
50 mg	¥ 3,630	现货
100 mg	¥ 4,870	现货
200 mg	¥ 6,570	现货
1 mL x 10 mM (in DMSO)	¥ 1,160	现货

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纯度: 99.13%

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COA HPLC HNMR 产品操作手册

产品介绍

Org 25543 AI Summary

Org 25543 displays significant inhibition of human Glycine Transporter type-2 (GlyT2) with IC50 values reported at 16.0 nM and 3.8 nM in different assays, showing strong efficacy in reducing [3H]glycine uptake in CHO cells and recombinant human GlyT2a. It also demonstrates weak inhibition of human Glycine Transporter type-1 (GlyT1) with an IC50 value greater than 100.0 nM in some assays, though another assay reports an IC50 of 22.0 nM for displacing [3H]glycine from GlyT1. Known for selective inhibition, this compound induces a significant increase in extracellular glycine levels in rat spinal cord neurons and shows antiallodynic and analgesic effects in mouse models, with a maximum tolerated dose of 2.0 mg/kg. Additionally, Org 25543 has antiviral activity against SARS-CoV-2, reducing cytotoxicity in Caco-2 and VERO-6 cells at certain concentrations. It also weakly inhibits human HDAC6 enzyme activity but shows moderate inhibition of the SARS-CoV-2 3CL-Pro protease. Lastly, in vivo receptor occupancy studies indicate dose-dependent engagement with GlyT2..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Org 25543 is the development of an N-Acyl amino acid that selectively inhibits the glycine transporter 2 to produce analgesia in a rat model of chronic pain.

化学信息

分子量	412.52
分子式	C₂₄H₃₂N₂O₄
CAS No.	363628-88-0
Smiles	O(CC1=CC=CC=C1)C2=C(OC)C=C(C(NCC3(N(C)C)CCCC3)=O)C=C2OC
密度	1.16 g/cm3 (Predicted)
颜色	Transparent
物理性状	Liquid

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: 55 mg/mL (133.33 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4241 mL	12.1206 mL	24.2412 mL	121.2062 mL
5 mM	0.4848 mL	2.4241 mL	4.8482 mL	24.2412 mL
10 mM	0.2424 mL	1.2121 mL	2.4241 mL	12.1206 mL
20 mM	0.1212 mL	0.6060 mL	1.2121 mL	6.0603 mL
50 mM	0.0485 mL	0.2424 mL	0.4848 mL	2.4241 mL
100 mM	0.0242 mL	0.1212 mL	0.2424 mL	1.2121 mL