VU-1545

Name: VU-1545
Brand: TargetMol
SKU: T23514
Price: 278 CNY
Availability: InStock
Rating: 5 (10 reviews)

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货号 T23514Cas号 890764-63-3

别名 VU 1545

VU-1545 是一种代谢型谷氨酸受体 5 正变构调节剂，Ki 为 156 nM，EC50为 9.6 nM。

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VU-1545

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纯度: 98.8%

货号 T23514 别名 VU 1545Cas号 890764-63-3

VU-1545 是一种代谢型谷氨酸受体 5 正变构调节剂，Ki 为 156 nM，EC50为 9.6 nM。

规格	价格	库存
1 mg	¥ 278	现货
2 mg	¥ 396	现货
5 mg	¥ 672	现货
10 mg	¥ 1,070	现货
25 mg	¥ 1,780	现货
50 mg	¥ 2,650	现货
100 mg	¥ 3,710	现货
200 mg	¥ 4,930	现货

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产品介绍

VU-1545 AI Summary

VU-1545 demonstrates significant bioactivities across a range of biological targets and systems. It shows notable affinity for the mGluR5 receptor, with a Ki value of 160.0 nM, suggesting competitive binding, and an EC50 value of 9.6 nM in enhancing glutamate-induced calcium flux in rat astrocytes, indicating its modulatory effect on receptor signaling. In addition to mGluR5, VU-1545 exhibits various biopotencies, including moderate activity in mitochondrial dynamics, lipid storage modulation, strong inhibition against AmpC Beta-Lactamase, ELG1-dependent DNA repair, and delayed death inhibition of the malarial parasite plastid. It also shows potential as an inhibitor of Nrf2, TGF-b, Hepatitis C Virus (HCV), GLP-1 receptor inverse agonist, human TDP1, and stage-specific inhibition of Vaccinia Orthopoxvirus. In antiviral assays, VU-1545 inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells by 9.16% at 10 µM concentration after 48 hours and shows potential inhibition of SARS-CoV-2 3CL-Pro protease by -2.219% at 20 µM. It also demonstrates activity in reducing SARS-CoV-2 induced cytotoxicity in VERO-6 cells by 0.36% at 10 µM concentration after 48 hours. Further, VU-1545 shows an inhibitory effect on human HDAC6 enzymatic activity, with 73.61% inhibition using a commercial peptide substrate. It impacts cell viability variably in HEK293T and U2OS cell lines, promoting growth, whereas it has mixed effects on human fibroblast cells. VU-1545 also affects the thermal stability of different molecular domains, either stabilizing or destabilizing them to varying extents. Moreover, it is active in GPCR β-arrestin recruitment assays with multiple targets, including GPR119, APLNR, ADRB2, FPR2, GLP1R, CX3CR1, AGTR1, ADGRF1, S1PR1, C5AR1, FFAR4, GPR35, and ADRA2A, showing diverse levels of activation and inhibition. This broad spectrum of activity highlights VU-1545's potential as a versatile bioactive molecule with applications in various therapeutic areas..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	VU-1545 is mGlu5 positive allosteric modulator.
靶点活性	mGluR5:156 nM (Ki), mGluR5:9.6 nM (EC50)
别名	VU 1545

化学信息

分子量	402.38
分子式	C₂₂H₁₅FN₄O₃
CAS No.	890764-63-3
Smiles	[O-][N+](=O)c1ccc(cc1)C(=O)Nc1cc(nn1-c1ccccc1F)-c1ccccc1
密度	1.34 g/cm3 (Predicted)
颜色	Yellow
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: 50 mg/mL (124.26 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4852 mL	12.4261 mL	24.8521 mL	124.2606 mL
5 mM	0.4970 mL	2.4852 mL	4.9704 mL	24.8521 mL
10 mM	0.2485 mL	1.2426 mL	2.4852 mL	12.4261 mL
20 mM	0.1243 mL	0.6213 mL	1.2426 mL	6.2130 mL
50 mM	0.0497 mL	0.2485 mL	0.4970 mL	2.4852 mL
100 mM	0.0249 mL	0.1243 mL	0.2485 mL	1.2426 mL