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Formula | C23H20FNO5 |
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Molecular Weight | 409.41 | CAS No. | 1078166-57-0 | |
Solubility (25°C)* | In vitro | 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1. | ||
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Targets |
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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] |
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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] |
Animal Study: |
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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 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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