PF-915275 - CAS:857290-04-1

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PF-915275

目录号 : KM14518 CAS No. : 857290-04-1 纯度 : 98%

Data Sheet 产品使用指南

PF-915275 是一种有效的，选择性的，具有口服活性的人 11β-羟基类固醇脱氢酶1型 (11βHSD1) 抑制剂，K_i 为 2.3 nM，EC₅₀ 为 15 nM (在 HEK293 细胞中)。PF-915275 对人和猴原代肝细胞中可的松向皮质醇的转化具有剂量依赖性，其 EC₅₀ 分别为 20 nM 和 100 nM。

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10mg		In-stock
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生物活性

PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a K_i of 2.3 nM and an EC₅₀ of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC₅₀ of 20 and 100 nM, respectively.

体外研究

PF-915275 is a potent inhibitor of 11βHSD1 (in vitro HEK293, EC₅₀ of 15 nM) in this human 11βHSD1 overexpressed cell line when coincubated in the presence of 300 nM enzyme substrate. Consistent with the species differences between human and rodent observed in biochemical assays, PF-915275 is a poor inhibitor of 11βHSD1 in rat FAO hepatoma cells, with an EC₅₀ of 14,500 nM. PF-915275 demonstrates species-dependent potency for inhibiting cellular conversion of cortisone to cortisol in dog, monkey, and human in primary hepatocytes, with activity in human hepatocytes/monkey hepatocytes/dog hepatocytes. PF-915275 does not significantly inhibit 11βHSD2 (only 1.5% inhibition when tested at 10 μM). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC₅₀ of 20 and 100 nM, respectively.

体内研究

The inhibition of either cortisone or prednisone turnover with PF-915275 yields similar EC₅₀ values to that in human hepatocytes (EC₅₀ by PF-915275 is 18 and 13 nM using cortisone and prednisone substrates, respectively) in vivo 11βHSD1 activity.
PF-915275 dose-dependently inhibits 11βHSD1-mediated conversion of prednisone to prednisolone. A maximum of 87% inhibition is observed, with the highest tested dose of 3 mg/kg.
The half-life of PF-915275 is 22 hours in monkey.
PF-915275 (0.1-3 mg/kg; oral administration; for 8 hours; male cynomolgus monkeys) treatment shows a trend in dose-dependent lowering of fed plasma insulin after 8 h of dosing in these monkeys. Plasma insulin levels are significantly lowered (by 54 and 60%, respectively) at 1 and 3 mg/kg PF-915275 treatment. Plasma glucose or lipid levels are not altered with treatment.

Animal Model:	Adult male cynomolgus monkeys (2-5 kg)
Dosage:	0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration:	Oral administration; for 8 hours
Result:	There was a trend in dose-dependent lowering of fed plasma insulin after 8 h of dosing in these monkeys. Plasma insulin levels were significantly lowered (by 54 and 60%, respectively).

分子式

C₁₈H₁₄N₄O₂S

分子量

350.39

CAS号

857290-04-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 31 mg/mL (88.47 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8540 mL	14.2698 mL	28.5396 mL
5 mM	0.5708 mL	2.8540 mL	5.7079 mL
10 mM	0.2854 mL	1.4270 mL	2.8540 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.83 mg/mL (2.37 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.37 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.83 mg/mL (2.37 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.37 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.83 mg/mL (2.37 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。