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

L-798106  (Synonyms: CM9; GW671021)

Cat. No.: HY-15274 Purity: 99.85%
COA Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 153 In-stock
Solution
10 mM * 1 mL in DMSO USD 153 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 205 In-stock
25 mg USD 420 In-stock
50 mg USD 675 In-stock
100 mg USD 1080 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (18.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8641 mL 9.3207 mL 18.6414 mL
5 mM 0.3728 mL 1.8641 mL 3.7283 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.85%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8641 mL 9.3207 mL 18.6414 mL 46.6035 mL
5 mM 0.3728 mL 1.8641 mL 3.7283 mL 9.3207 mL
10 mM 0.1864 mL 0.9321 mL 1.8641 mL 4.6604 mL
15 mM 0.1243 mL 0.6214 mL 1.2428 mL 3.1069 mL
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L-798106 Related Classifications

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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