| Identification | Back Directory | [Name]
N-[(5-Bromo-2-methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylmethyl)phenyl]-2-propenamide | [CAS]
244101-02-8 | [Synonyms]
CM 9
GW 671021
L-798,106
N-[(5-Bromo-2-methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylmethyl)phenyl]-2-propenamide
(2E)-N-[(5-BroMo-2-Methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylMethyl)phenyl]-2-propenaMide
2-Propenamide, N-[(5-bromo-2-methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylmethyl)phenyl]-, (2E)- | [Molecular Formula]
C27H22BrNO4S | [MDL Number]
MFCD08272644 | [MOL File]
244101-02-8.mol | [Molecular Weight]
536.44 |
| Chemical Properties | Back Directory | [density ]
1.425±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: >20mg/mL | [form ]
powder | [pka]
4.26±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
L-798106 is a potent and selective prostanoid receptor EP3-selective antagonists. L-798106 has been used in multiple studies to tease out EP3 agonist activity, both in vitro and in vivo. L-798106 successfully blocks the actions of sulprostone, an EP3-selective agonist. L-798106 was useful in showing that the vascular contraction effect of PGE2 is due to its prostanoid EP3 agonist activity. | [Uses]
L-798106, a selective prostanoid receptor EP3 antagonist, is used in prostanoid receptor signaling studies that regulate COX-2 levels and the central excitatory effects of PGE(2) on PVN neurons. | [Definition]
ChEBI: L-798106 is an N-sulfonylcarboxamide resulting from the formal condensation of the carboxy group of o-naphthalen-2-ylcinnamic acid with the sulfonamide group of 5-bromo-2-methoxybenzenesulfonamide. It is a selective antagonist for the prostanoid receptor EP3, a prostaglandin receptor for prostaglandin E2 (PGE2). It has a role as a prostaglandin receptor antagonist. It is a N-sulfonylcarboxamide, a member of bromobenzenes and an aromatic ether. | [Biochem/physiol Actions]
L-798106 was among the first prostanoid receptor EP3-selective antagonists. It has been used in multiple studies to tease out EP3 agonist activity, both in vitro and in vivo. It successfully blocks the actions of sulprostone, an EP3-selective agonist, and it helped show that the vascular contraction effect of PGE2 is due to its prostanoid EP3 agonist activity. | [in vivo]
L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation in db/db mice[3]. | Animal Model: | Male db/db mice[3] | | Dosage: | 50 and 100 μg/kg | | Administration: | Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks | | Result: | Suppressed the increased fasting blood glucose levels in the db/db mice.
Suppressed increased proinflammatory gene expressions in the adipocytes isolated from the epididymal AT of the db/db mice. |
| [IC 50]
EP3: 0.3 nM (IC50); EP4: 916 nM (IC50); EP1: >5000 nM (IC50); EP2: >5000 nM (IC50) | [storage]
Store at RT |
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