E-7046
- Product Name
- E-7046
- CAS No.
- 1369489-71-3
- Chemical Name
- E-7046
- Synonyms
- CPD1542;E-7046;AN-0025;Palupiprant;ER-886046-00;E-7046,E7046;E7046 (ER-886406);E-7046;E 7046;E7046;Inhibitor,E-7046,Prostaglandin Receptor,E7046,E 7046,inhibit;(S)-4-(1-(3-(difluoromethyl)-1-methyl-5-(3-(trifluoromethyl)phenoxy)-1H-pyrazole-4-carboxamido)ethyl)benzoic acid
- CBNumber
- CB23168471
- Molecular Formula
- C22H18F5N3O4
- Formula Weight
- 483.39
- MOL File
- 1369489-71-3.mol
E-7046 Property
- Boiling point:
- 594.8±50.0 °C(Predicted)
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- ≤12mg/ml in ethanol;14mg/ml in DMSO;2mg/ml in dimethyl formamide
- form
- crystalline solid
- pka
- 4.17±0.10(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 19673
- Product name
- E7046
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 19673
- Product name
- E7046
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $84
- Updated
- 2024/03/01
- Product number
- 19673
- Product name
- E7046
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $193
- Updated
- 2024/03/01
- Product number
- 19673
- Product name
- E7046
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $321
- Updated
- 2024/03/01
- Product number
- E102400
- Product name
- E-7046
- Packaging
- 5mg
- Price
- $125
- Updated
- 2021/12/16
E-7046 Chemical Properties,Usage,Production
Uses
E-7046 is an orally bioavailable and specific EP4 antagonist and exhibits anti-tumor activity. EP4 antagonists reverse PGE2-induced suppression of TNFα production in human whole blood.
Biological Activity
e7046 is a potent and selective antagonist that potently competes with pge2 binding to the type 4 prostaglandin e2 (pge2) receptor ep4 [1,2].prostaglandin e2 receptor 4 (ep4) is a prostaglandin receptor for prostaglandin e2 (pge2) implicated in various physiological and pathological responses in animal models and humans [3].
in vivo
in apcmin/+ mice, daily oral administration of e7046 slowed down the growth of established subcutaneous tumors and significantly delayed the recurrence of tumors after surgical resection. e7046 significantly reduced the combined colon polyp area and the size of individual polyps without influencing the total polyp number. e7046 exhibited great activity against colon and small intestine tumors [1]. e7046 delayed the growth of multiple syngeneic murine tumor types. e7046 showed no effect on tumor cell viability in vitro [2]. in the ct26 model, treatment with e7046 and anti-pd1 inhibited tumor growth. in the 4t1 model, e7046 in combination with anti-ctla4 resulted in a nearly complete tumor growth inhibition [4].
References
[1] albu d i, wu j, huang k, et al. abstract b198: pharmacological profile of the pge2 ep4 receptor antagonist e7046[j]. 2015.
[2] albu d i, huang k c, wu j, et al. abstract b034: preclinical immune antitumor activity of myeloid-targeting e7046 and treg depleting e7777[j]. 2016.
[3] negishi m, sugimoto y, ichikawa a. prostaglandin e receptors[j]. journal of lipid mediators and cell signalling, 1995, 12(2-3): 379-391.
[4] bao x, albu d, huang k c, et al. combination of ep4 antagonist and checkpoint inhibitors promotes anti-tumor effector t cells in preclinical tumor models[j]. journal for immunotherapy of cancer, 2015, 3(2): p350.
E-7046 Preparation Products And Raw materials
Raw materials
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