PF-04418948

製品コードS7211 バッチS721102

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₃H₂₀FNO₅

分子量

409.41

CAS No.

1078166-57-0

Solubility (25°C)*

体外

DMSO

82 mg/mL (200.28 mM)

Ethanol

3 mg/mL (7.32 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5% DMSO 1 95% Corn oil	0.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.1mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.
in vitro	PF-04418948 antagonizes the effects of butaprost and PGE2 on an EFS-induced contraction of the human myometrium, and antagonizes PGE2-induced relaxation of carbachol pre-contracted rings of mouse trachea. ^[1] PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively. ^[2] PF-04418948 restores neutrophil extracellular traps (NETs) formation in neutrophils isolated from BMT mice or HSCT patients. ^[3]
in vivo	In Rats, PF-04418948 (10 mg/kg, p.o.) reduces the mean cutaneous blood flow peak response and AUC_0–60 by 41% and 61%, respectively. ^[1]

製品説明

PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.

in vitro

PF-04418948 antagonizes the effects of butaprost and PGE2 on an EFS-induced contraction of the human myometrium, and antagonizes PGE2-induced relaxation of carbachol pre-contracted rings of mouse trachea. ^[1]

PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively. ^[2]

PF-04418948 restores neutrophil extracellular traps (NETs) formation in neutrophils isolated from BMT mice or HSCT patients. ^[3]

in vivo

In Rats, PF-04418948 (10 mg/kg, p.o.) reduces the mean cutaneous blood flow peak response and AUC_0–60 by 41% and 61%, respectively. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	16 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Sprague Dawley rats
	投薬量	10 mg/kg
	投与方法	p.o.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Paradoxical Induction of ALOX15/15B by Cortisol in Human Amnion Fibroblasts: Implications for Inflammatory Responses of the Fetal Membranes at Parturition [ Int J Mol Sci, 2023, 24(13)10881]	PubMed: 37446059
Dual Blockade of EP2 and EP4 Signaling is Required for Optimal Immune Activation and Antitumor Activity Against Prostaglandin-Expressing Tumors [ Cancer Res Commun, 2023, 3(8):1486-1500]	PubMed: 37559947
Dual Blockade of EP2 and EP4 Signaling is Required for Optimal Immune Activation and Antitumor Activity Against Prostaglandin-Expressing Tumors [ Cancer Res Commun, 2023, 3(8):1486-1500]	PubMed: 37559947
PGE2 activates EP4 in subchondral bone osteoclasts to regulate osteoarthritis [ Bone Res, 2022, 10(1):27]	PubMed: 35260562
Identification of a feed-forward loop between 15-S-HETE and PGE2 in human amnion at parturition [ J Lipid Res, 2022, S0022-2275-2200127-4]	PubMed: 36206855
The cyclooxygenase-1/mPGES-1/endothelial prostaglandin EP4 receptor pathway constrains myocardial ischemia-reperfusion injury. [ Nat Commun, 2019, 10(1):1888]	PubMed: 31015404
Protective Role of mPGES-1 (Microsomal Prostaglandin E Synthase-1)-Derived PGE2 (Prostaglandin E2) and the Endothelial EP4 (Prostaglandin E Receptor) in Vascular Responses to Injury. [ Arterioscler Thromb Vasc Biol, 2018, 38(5):1115-1124]	PubMed: 29599139

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。