受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H20FNO5 |
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分子量 | 409.41 | CAS No. | 1078166-57-0 | |
Solubility (25°C)* | 体外 | DMSO | 81 mg/mL (197.84 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
製品説明 | PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1. |
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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 AUC0–60 by 41% and 61%, respectively. [1] |
細胞アッセイ | 細胞株 | Cell-free assays |
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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. |
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。