1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. L-902688

L-902688 

Cat. No.: HY-119163
Handling Instructions

L-902688 is a potent, selective and orally active EP4 receptor agonist with a Ki of 0.38 nM and an EC50 of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors.

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

L-902688 Chemical Structure

L-902688 Chemical Structure

CAS No. : 634193-54-7

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Description

L-902688 is a potent, selective and orally active EP4 receptor agonist with a Ki of 0.38 nM and an EC50 of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors[1][2].

IC50 & Target[2]

EP4

0.38 nM (Ki)

EP4

0.6 nM (EC50)

In Vitro

L-902688 (1 µM; 24 hours; HUVE cells) treatment attenuates TGF-β-induced Twist and α-smooth muscle actin (α-SMA) expression[1].

Western Blot Analysis[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: 1 µM
Incubation Time: 24 hours
Result: Attenuated TGF-β-induced Twist and α-smooth muscle actin (α-SMA) expression.
In Vivo

L-902688 (0.25-1 µg/kg/day; intraperitoneal injection; daily; for 3 weeks; adult male Sprague-Dawley rats) treatment reduces right ventricle fibrosis in the monocrotaline (MCT)-induced PAH rat model[1].

Animal Model: Adult male Sprague-Dawley rats injected with crotaline to induce pulmonary arterial hypertension (PAH) and right ventricular (RV) hypertrophy[1]
Dosage: 0.25 µg/kg/day, 0.4 µg/kg/day or 1 µg/kg/day
Administration: Intraperitoneal injection; daily; for 3 weeks
Result: Reduced right ventricle fibrosis in the monocrotaline (MCT)-induced PAH rat model.
Molecular Weight

419.47

Formula

C₂₁H₂₇F₂N₅O₂

CAS No.

634193-54-7

SMILES

O[[email protected]@]([H])(C(F)(C1=CC=CC=C1)F)/C=C/[[email protected]@H](CCC2=O)N2CCCCCCC3=NN=NN3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

L-902688L902688L 902688Prostaglandin ReceptorEP4α-SMAcardiacfibrosisTwistTGF-βendothelial-mesenchymaltransitionInhibitorinhibitorinhibit

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L-902688
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HY-119163
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