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Grapiprant

Grapiprant

Product ID G681019
Cas No. 415903-37-6
Purity ≥98%
Product Unit SizeCostQuantityStock
5 mg $108.00 In stock
25 mg $328.50 In stock
100 mg $871.00 In stock
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  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Description
  • Product Info
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  • Downloads
  • References
  • Custom Order

Description

Grapiprant is an orally bioavailable antagonist of the prostaglandin E receptor subtype 4 (EP4), with potential analgesic, immunomodulating and antineoplastic activities. Upon administration of grapiprant, this agent selectively binds to and inhibits the binding of prostaglandin E2 (PGE2) and prevents the activation of the EP4 receptor. This inhibits PGE2-EP4 receptor-mediated signaling and prevents proliferation in tumor cells in which the PGE2-EP4 signaling pathway is over-activated. In addition, EP4 receptor inhibition modulates the immune system by preventing both interleukin-23 (IL-23) production and the IL-23-mediated expansion of Th17 cells. As EP4 is expressed by peripheral sensory neurons, blockade of EP4-mediated signaling may induce an analgesic effect. EP4, a prostanoid receptor subtype, is a G protein-coupled receptor that is expressed in certain types of cancers; it promotes tumor cell proliferation and invasion.
NCI Thesaurus (NCIt)

Product Info

Cas No.

415903-37-6

Purity

≥98%

Formula

C26H29N5O3S

Formula Wt.

491.61

Chemical Name

1-[2-[4-(2-ethyl-4,6-dimethylimidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea

IUPAC Name

1-[2-[4-(2-ethyl-4,6-dimethylimidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea

Synonym

CJ-023423; RQ-00000007; AAT-007

Solubility

DMSO (>80 mg/mL), ethanol (>20 mf/mL). Insoluble in water..

Shipping and Storage

Store Temp

-20°C

Ship Temp

Ambient

Downloads

Info Sheet

G681019 Info Sheet PDF

References

Shaw  KK,  Rausch-Derra  LC , Rhodes L. Grapiprant: an EP4 prostaglandin receptor antagonist and novel therapy for pain and inflammation. V. med Sci. (2015) 2:3-9. PMID: 29067176 PMCID: PMC5645826 DOI: 10.1002/vms3.13

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