1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. L-798106

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.

For research use only. We do not sell to patients.

L-798106 Chemical Structure

L-798106 Chemical Structure

CAS No. : 244101-02-8

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10 mM * 1 mL in DMSO In-stock
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Description

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[1].

IC50 & Target

EP3

0.3 nM (IC50)

EP4

916 nM (IC50)

EP1

>5000 nM (IC50)

EP2

>5000 nM (IC50)

In Vitro

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.

Cell Viability Assay[2]

Cell Line: Guinea-pig vas deferens
Concentration: 200 nM
Incubation Time:
Result: Showed an apparent pA2 of 7.48±0.25.

Cell Viability Assay[2]

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).
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

536.44

Formula

C27H22BrNO4S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NS(=O)(C1=CC(Br)=CC=C1OC)=O)/C=C/C2=CC=CC=C2CC3=CC=C4C=CC=CC4=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 99.81%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
L-798106
Cat. No.:
HY-15274
Quantity:
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