L-798106
Based on 1 publication(s) in Google Scholar
L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM, respectively.
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- Reinheit: 99.91%
- CAS. Nr.: 244101-02-8
- Formel: C27H22BrNO4S
- Molecular Weight:536.44
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) L-798106
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Biologische Aktivität
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EP3 0.3 nM (Ki) |
EP4 916 nM (Ki) |
EP1 >5000 nM (Ki) |
EP2 >5000 nM (Ki) |
L-798106 (200 nM) inhibits electrical field stimulation-induced contractile responses[2].
L-798106 (10 μM) inhibits electrical field stimulation-evoked ACh release[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Guinea-pig vas deferens
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Concentration:200 nM
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Incubation Time:
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Result:Showed an apparent pA2 of 7.48±0.25.
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Cell Line:Guinea-pig tracheal smooth muscle
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Concentration:10 μM
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Incubation Time:
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Result:Attenuated significantly the inhibitory effect of all agents tested (in % inhibition of EFS-induced release: 8-iso-PGE1 from 56.9 to 8.6; 8-iso-PGE2 from 51.6 to 9.2; PGE2 from 61.2 to 2.9; sulprostone from 55.9 to 18.8).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male db/db mice[3]
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Dosage:50 and 100 μg/kg
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Administration:Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks
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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.
Chemical Information
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CAS. Nr. 244101-02-8
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Appearance Solid
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Molecular Weight 536.44
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Formel C27H22BrNO4S
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Color White to off-white
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SMILES
O=C(NS(=O)(C1=CC(Br)=CC=C1OC)=O)/C=C/C2=CC=CC=C2CC3=CC=C4C=CC=CC4=C3
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Synonyms
CM9; GW671021
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Neurogastroenterol Motil
Shugan Decoction Ameliorated WAS-Induced Abnormal Colonic Motility in Rats by Inhibiting Colonic TRPV4-PGE2 Signaling. [Abstract]2025 Dec;37(12):e70104. PMID: 40545667
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Juteau H, et al. Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor. Bioorg Med Chem. 2001 Aug;9(8):1977-84. [Content Brief]
[2]. Deborah L Clarke, et al. E-ring 8-isoprostanes inhibit ACh release from parasympathetic nerves innervating guinea-pig trachea through agonism of prostanoid receptors of the EP3-subtype. Br J Pharmacol. 2004 Feb;141(4):600-9. [Content Brief]
[3]. Pei-Chi Chan, et al. Importance of adipocyte cyclooxygenase-2 and prostaglandin E2-prostaglandin E receptor 3 signaling in the development of obesity-induced adipose tissue inflammation and insulin resistance. FASEB J. 2016 Jun;30(6):2282-97. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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