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L-798106
CAS No. 244101-02-8
L-798106( —— )
Catalog No. M33398 CAS No. 244101-02-8
L-798106 (CM9) is a selective and potent prostaglandin-like EP3 receptor antagonist that inhibits EP4, EP1, and EP2 receptors, suppresses levels of pro-inflammatory cytokines in atherosclerosis, and attenuates PGE2-induced cough.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 101 | In Stock |
|
| 10MG | 160 | In Stock |
|
| 25MG | 330 | In Stock |
|
| 50MG | 519 | In Stock |
|
| 100MG | 830 | In Stock |
|
| 200MG | 1097 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameL-798106
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NoteResearch use only, not for human use.
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Brief DescriptionL-798106 (CM9) is a selective and potent prostaglandin-like EP3 receptor antagonist that inhibits EP4, EP1, and EP2 receptors, suppresses levels of pro-inflammatory cytokines in atherosclerosis, and attenuates PGE2-induced cough.
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DescriptionL-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 of916 nM, >5000 nM and >5000 nM, respectively.
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In VitroL-798106 (200 nM) inhibits electrical field stimulation-induced contractile responses.L-798106 (10 μM) inhibits electrical field stimulation-evoked ACh release.Cell Viability Assay Cell Line:Guinea-pig vas deferens Concentration:200 nM Incubation Time:Result:Showed an apparent pA2 of 7.48±0.25.Cell Viability Assay Cell Line:Guinea-pig tracheal smooth muscle Concentration:10 μM Incubation Time: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).
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In VivoL-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation in db/db mice.Animal Model:Male db/db mice 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.
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Synonyms——
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PathwayGPCR/G Protein
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TargetProstaglandin Receptor
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RecptorProstaglandin Receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number244101-02-8
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Formula Weight536.44
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Molecular FormulaC27H22BrNO4S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 10 mg/mL (18.64 mM; Ultrasonic )
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SMILESCOc1ccc(Br)cc1S(=O)(=O)NC(=O)\C=C\c1ccccc1Cc1ccc2ccccc2c1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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.?
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