1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. CAY10471

CAY10471 (Synonyms: TM30089)

Cat. No.: HY-13706A
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CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model.

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CAY10471 Chemical Structure

CAY10471 Chemical Structure

CAS No. : 627865-18-3

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Description

CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model[1][2][3].

IC50 & Target[1]

hCRTH2

 

In Vitro

CAY10471 (1 μM; 1-24 hours) decreases 15dPGJ2-induced phosphorylation of p38 MAP kinase significantly in PC12 cells[1].

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 1 μM
Incubation Time: 1 or 24 hours
Result: Blocked 15d-PGJ2-induced p38 MAP kinase activation.
In Vivo

CAY10471 (oral treatment; 2 mg/kg; challenged on day 22 or over 10 consecutive days) shows a diminished inflammation in chronic contact hypersensitivity (CHS) and IgE-CAI model. It blocks CRTH2 partly, but significantly suppresses inflammation in mice[2].
CAY10471 (oral adminstration; 20 mg/kg; twice daily; beginning 3/4/5 days before UUO) significantly attenuates interstitial collagen deposition in the cortex when compared with the vehicle (8.40% versus 14.85%). Oral administration from 3 days after UUO also significantly attenuates interstitial collagen deposition in the cortex compared with vehicle (9.63% versus 14.44%). However, oral administration beginning 5 days after UUO has little effect on interstitial collagen deposition in the cortex when compared with vehicle (14.61% versus 15.09%). Unilateral ureteral obstruction (UUO)[3].

Animal Model: Balb/c mice, DP−/− mice, CRTH2−/− mice[2]
Dosage: 2 mg/kg
Administration: Oral treatment; once daily; challenged on day 22 or over 10 consecutive days
Result: Significantly suppressed both CHS and IgE-CAI inflammatory responses.
Animal Model: C57BL/6 mice[3]
Dosage: 20 mg/kg
Administration: Oral treatment; twice daily; beginning 3/4/5 days before UUO
Result: Slowed the progression of renal fibrosis in the obstructed kidneys.
Molecular Weight

416.47

Formula

C₂₁H₂₁FN₂O₄S

CAS No.

627865-18-3

SMILES

O=C(CN1C2=C(CC(CC2)N(C)S(=O)(C3=CC=C(C=C3)F)=O)C4=C1C=CC=C4)O.[Rotation (+)]

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

CAY10471TM30089CAY 10471CAY-10471TM 30089TM-30089Prostaglandin ReceptorchronicskininflammationcontacthypersensitivityCHSPC12cellstubulointerstitialfibrosisInhibitorinhibitorinhibit

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