GLP-1R Antagonist 1

Name: GLP-1R Antagonist 1
Brand: TargetMol
SKU: T15387
Rating: 4.5 (1 reviews)

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货号 T15387Cas号 488097-06-9

GLP-1R Antagonist 1 (compound 5d) 是口服有效的、能透过中枢神经系统的，胰高血糖素样肽 1 受体 (GLP-1R) 的非竞争性抑制，其 IC50 值为 650 nM。

GLP-1R Antagonist 1

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纯度: 99.84%

货号 T15387Cas号 488097-06-9

GLP-1R Antagonist 1 (compound 5d) 是口服有效的、能透过中枢神经系统的，胰高血糖素样肽 1 受体 (GLP-1R) 的非竞争性抑制，其 IC50 值为 650 nM。

规格	价格	库存	数量
1 mg	¥ 413	待询

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产品介绍

GLP-1R Antagonist 1 AI Summary

GLP-1R Antagonist 1 demonstrates a diverse range of bioactivities, including inhibition of several biological processes such as Lamin A splicing, S1P2 receptor antagonism, Luciferase translation or activity, Rab9 promoter activation, and SMN2 splice variant expression. It also affects ROR gamma transcriptional activity, prion and alpha-synuclein mRNA translation, ELG1-dependent DNA repair, and the functionality of malarial parasite plastids. The compound shows selective cytotoxicity in NF-kB activation-related cell lines and is active in cytochrome panel assays. Additionally, GLP-1R Antagonist 1 is potent in inducing DNA re-replication, modulating PINK1 expression, and inhibiting hepatitis C virus and TGF-b signaling. It showcases activity in cell-based systems pertinent to bone formation, muscle dystrophy alleviation, and viral entry. Furthermore, GLP-1R Antagonist 1 acts as an antagonist at the human GLP-1 receptor, inhibiting GLP1-induced and exendin-4-induced cAMP accumulation with IC50 values around 650-690 nM. It presents moderate inhibition of CYP enzymes with IC50 values between 400-4100 nM. The compound has good oral bioavailability (50%) and a half-life of approximately 9.8 hours in Sprague-Dawley rats, although it shows minimal CNS penetration based on the brain-to-plasma drug level ratio. These characteristics suggest that GLP-1R Antagonist 1 has potential as a GLP-1 receptor antagonist with promising pharmacokinetic properties suitable for further development..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	GLP-1R Antagonist 1 is an orally active, CNS penetrant and non-competitive glucagon-like peptide 1 receptor (GLP-1R) antagonist (IC50: 650 nM).
靶点活性	GLP1 receptor:650 nM

化学信息

分子量	440.73
分子式	C₁₆H₁₁ClF₆N₄O₂
CAS No.	488097-06-9
Smiles	Cn1c2NC(=NC(c2c(=O)n(C)c1=O)(C(F)(F)F)C(F)(F)F)c1ccc(Cl)cc1
密度	no data available
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: 90 mg/mL (204.21 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 3.3 mg/mL (7.49 mM), Sonication is recommeded.

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

	1mg	5mg	10mg	50mg
1 mM	2.2690 mL	11.3448 mL	22.6896 mL	113.4481 mL
5 mM	0.4538 mL	2.2690 mL	4.5379 mL	22.6896 mL
10 mM	0.2269 mL	1.1345 mL	2.2690 mL	11.3448 mL
20 mM	0.1134 mL	0.5672 mL	1.1345 mL	5.6724 mL
50 mM	0.0454 mL	0.2269 mL	0.4538 mL	2.2690 mL
100 mM	0.0227 mL	0.1134 mL	0.2269 mL	1.1345 mL