PF-5190457

目录号: GC31478纯度: >98.50%同义词: PF-05190457

PF-5190457是一种有效，选择性的生长素释放肽受体(ghrelinreceptor)反向激动剂，pKi值为8.36。

Cas No.: 1334782-79-4

规格	价格	库存	数量
5mg	¥1,035.00	现货	1
10mg	¥1,818.00	现货	1
25mg	¥3,636.00	现货	1
50mg	¥6,181.00	现货	1
100mg	¥10,512.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
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Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.

PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity[1].

PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets[1].

[1]. Bhattacharya SK, et al. Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9.

实验参考方法 Experimental Reference Method

Cell experiment:

Human whole islets are incubated in assay buffer containing 2.8 mM glucose for 45 minutes at 37 °C to stabilize insulin secretion; islets are then treated with 11.2 mM glucose in the presence and absence of PF-5190457 for one hour at 37 °C. Following incubation, samples are tested for the amount of insulin secreted into the media[1].

References:

[1]. Bhattacharya SK, et al. Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号

1334782-79-4

同义词

PF-05190457

SMILES

CC1=NC=NC(C2=CC(CC[C@H]3N4CC5(CCN(C(CC6=CN7C=C(C)SC7=N6)=O)CC5)C4)=C3C=C2)=C1

分子式

C₂₉H₃₂N₆OS

分子量

512.67 g/mol

溶解性

DMSO: 250 mg/mL (487.64 mM)

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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体积 (Volume)

浓度 (Concentration)

分子量 (MW)

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