1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. KAG-308

KAG-308 

Cat. No.: HY-128686 Purity: 99.88%
COA Handling Instructions

KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.

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

KAG-308 Chemical Structure

KAG-308 Chemical Structure

CAS No. : 1215192-68-9

Size Price Stock Quantity
5 mg USD 1650 In-stock
10 mg USD 2650 In-stock
25 mg USD 5250 In-stock
50 mg USD 8700 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE KAG-308

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor[1].

IC50 & Target

EC50: 17 nM (Human EP4 receptor), 160 nM (Human EP3 receptor), 1000 nM (Human EP2 receptor), 1000 nM (Human EP2 receptor)[1]
Ki: 2.57 nM (Human EP4 receptor), 32.4 nM (Human EP3 receptor), 52.9 nM (Human IP receptor), 1410 nM (Human EP1 receptor), 1540 nM (Human EP2 receptor)[1]

In Vitro

KAG-308 is a potent selective and orally active agonist of EP4 receptor, suppresses colitis and promots histological mucosal healing. KAG-308 shows a Ki and EC50 values of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over human EP1 (Ki, 1410 nM; EC50, 1000 nM), EP2 (Ki, 1540 nM; EC50, 1000 nM), EP3 (Ki, 32.4 nM; EC50, 160 nM) and IP receptor (Ki, 52.9 nM; EC50, >10000 nM). KAG-308 also exhibits potent agonist activity for human and mouse EP4 with an EC50 of 0.15 nM and 1.0 nM, respectively in the dual luciferase reporter assay[1].

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

Molecular Weight

460.52

Formula

C24H30F2N4O3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O[C@H](C1)[C@H](/C=C/[C@@H](O)[C@@H](C2=CC=CC(C)=C2)C)[C@](C/3(F)F)([H])[C@@]1([H])OC3=C/CCCC4=NN=NN4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 80 mg/mL (173.72 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1715 mL 10.8573 mL 21.7146 mL
5 mM 0.4343 mL 2.1715 mL 4.3429 mL
10 mM 0.2171 mL 1.0857 mL 2.1715 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 6 mg/mL (13.03 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 6 mg/mL (13.03 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.88%

References
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KAG-308 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:
KAG-308
Cat. No.:
HY-128686
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