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.
Product information
CAS Number: 627865-18-3
Molecular Weight: 416.47
Formula: C21H21FN2O4S
Chemical Name: (+)-2-[3-(N-methyl4-fluorobenzenesulfonamido)-2, 3, 4, 9-tetrahydro-1H-carbazol-9-yl]acetic acid
Smiles: CN(C1CC2=C(CC1)N(CC(O)=O)C1=CC=CC=C21)S(=O)(=O)C1C=CC(F)=CC=1
InChiKey: CANCTKXGRVNXFP-UHFFFAOYSA-N
InChi: InChI=1S/C21H21FN2O4S/c1-23(29(27,28)16-9-6-14(22)7-10-16)15-8-11-20-18(12-15)17-4-2-3-5-19(17)24(20)13-21(25)26/h2-7,9-10,15H,8,11-13H2,1H3,(H,25,26)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CAY10471 (1 μM; 1-24 hours) decreases 15dPGJ2-induced phosphorylation of p38 MAP kinase significantly in PC12 cells.
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. 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).
Products are for research use only. Not for human use.
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