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PF-06291874

Name: PF-06291874
Brand: TargetMol
SKU: TQ0239
Price: 248 CNY
Availability: InStock
Rating: 5 (10 reviews)

Synonyms: Glucagon receptor antagonists-4

货号 TQ0239Cas号 1393124-08-7 一键复制产品信息纯度: 99.27%

很棒

PF-06291874 (Glucagon receptor antagonists-4) 是口服有活性的胰高血糖素受体非肽类拮抗剂。它正用于研究 2 型糖尿病。

PF-06291874

一键复制产品信息

很棒

纯度: 99.27%

货号 TQ0239Cas号 1393124-08-7

别名 Glucagon receptor antagonists-4

PF-06291874 (Glucagon receptor antagonists-4) 是口服有活性的胰高血糖素受体非肽类拮抗剂。它正用于研究 2 型糖尿病。

规格	价格	库存
1 mg	¥ 248	现货
5 mg	¥ 578	现货
10 mg	¥ 828	现货
25 mg	¥ 1,830	现货
50 mg	¥ 3,230	现货
1 mL x 10 mM (in DMSO)	¥ 647	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。 凭借在化合物合成方面的丰富经验，我们可以根据您的研究需求为该产品提供快速定制合成服务.

实验操作小课堂

常见问题解答

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纯度: 99.27%

颜色: 白色

性状: Solid

资源下载: COA LCMS HNMR 产品操作手册

产品介绍

PF-06291874 AI Summary

PF-06291874 exhibits a diverse range of bioactivities, including significant permeability properties, receptor binding affinities, and varied inhibitory and modulatory effects across multiple cell types and receptors. It demonstrates apparent permeability across MDCK2 cells (Papp 3.6 ucm/s) and human Caco-2 cells (Papp 30.0 ucm/s at pH 6.5 and 8.5 ucm/s at pH 7.4), as well as across dog RRCK cells (8.5 x 10^-6 cm/s). It acts as an antagonist at various glucagon receptors in species including human, monkey, dog, mouse, and rats, with Kb values from 82.0 nM to 3900.0 nM, and displaces [125I]-glucagon-cex from the human glucagon receptor with a Ki value of 14.0 nM. The compound shows specific binding affinity to GLP-1 receptors (Ki 3160.0 nM) and inhibits the rat GABA-gated chloride channel (Ki 8200.0 nM). In terms of pharmacokinetics, PF-06291874 has 100% oral bioavailability in both Beagle dogs (5 mg/kg, half-life 2.5 hours, Vdss 0.31 L/kg) and Wistar-Han rats (50 mg/kg, half-life 1.8 hours, Vdss 0.4 L/kg). It also shows plasma clearance rates in Beagle dogs (1.5 mL/min/kg) and Wistar-Han rats (2.8 mL/min/kg). With a log D value of 2.5 at pH 7.4, the compound also demonstrates significant cytotoxicity against human THLE cells (IC50 112000.0 nM). Additionally, PF-06291874 shows cell type-dependent effects on cell viability, with varying growth rates in HEK293T, U2OS, and human fibroblast cells. Thermal Shift Assay results indicate that it has both stabilizing and destabilizing effects on different protein domains. Notably, it has a broad spectrum of GPCR activities, showing positive modulation on GPR119 (2.783% maximal response), and inhibitory effects on CX3CR1, ADRB2, APLNR, FPR2, ADRA2A, C5AR1, and S1PR1 among others, with varying levels of inhibition. Furthermore, it exhibits both maximal response and inhibition at different concentrations on targets like FFAR4, AGTR1, GPR35, and GLP1R, thus highlighting its extensive and diverse bioactivity profile..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	PF-06291874 (Glucagon receptor antagonists-4) (Glucagon receptor antagonists-4) is a highly effective and orally active antagonist of the glucagon receptor.
别名	Glucagon receptor antagonists-4

化学信息

分子量	503.51
分子式	C₂₆H₂₈F₃N₃O₄
CAS No.	1393124-08-7
Smiles	CCC[C@H](Oc1cc(C)c(c(C)c1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O
密度	1.27 g/cm3 (Predicted)

储存&溶解度

存储

溶解度信息

DMSO: 30 mg/mL (59.58 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.97 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

	1mg	5mg	10mg	50mg
1 mM	1.9861 mL	9.9303 mL	19.8606 mL	99.3029 mL
5 mM	0.3972 mL	1.9861 mL	3.9721 mL	19.8606 mL
10 mM	0.1986 mL	0.9930 mL	1.9861 mL	9.9303 mL
20 mM	0.0993 mL	0.4965 mL	0.9930 mL	4.9651 mL
50 mM	0.0397 mL	0.1986 mL	0.3972 mL	1.9861 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。