E-7046 free base · Synonyms: Palupiprant

Palupiprant is an orally bioavailable and specific EP4 antagonist.

For research use only. Not for human or veterinary use.

Target Prostaglandin Receptor

Research area Endocrinology Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

E-7046 structure

CAS No.: 1369489-71-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 480.00	BP-01877-1g	In stock	Get quote
2 g	USD 780.00	BP-01877-2g	In stock	Get quote
5 g	USD 1,380.00	BP-01877-5g	In stock	Get quote
10 g	Inquire	BP-01877-10g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

Palupiprant (E7046) is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. Palupiprant exhibits anti-tumor activities.

Biological activity

In Vitro Palupiprant (E7046) reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells through selective EP4 antagonism. In Vivo In the CT-26 tumor model, the Palupiprant/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of Palupiprant and RT also produces significant better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors. Palupiprant (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. Blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. Palupiprant treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells. Furthermore, co-administration of Palupiprant and E7777, an IL-2-diphtheria toxin fusion protein that preferentially kills Tregs, synergistically disrupts the myeloid and Treg immunosuppressive networks, resulting in effective and durable anti-tumor immune responses in mouse tumor models.

Identifiers

SMILES: C[C@H](NC(=O)C1=C(OC2=CC=CC(=C2)C(F)(F)F)N(C)N=C1C(F)F)C1=CC=C(C=C1)C(O)=O
InChIKey: MKLKAQMPKHNQPR-NSHDSACASA-N

Specifications

MW (average): 483.3880
Formula: C₂₂H₁₈F₅N₃O₄
CAS No.: 1369489-71-3
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. X. Bao, et al. Combination of a Novel EP4 Antagonist E7046 and Radiation Therapy Promotes Anti-tumor Immune Response and Tumor Rejection in Preclinical Tumor Models. International Journal of Radiation Oncology Biology Physics

[2]. Diana I. Albu, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. OncoImmunology.

Same research area

Search Endocrinology