(+)-3-[[(4-Fluorophenyl)sulfonyl]methylamino]-1,2,3,4-tetrahydro-9H-carbazole-9-acetic acid

Product Name(+)-3-[[(4-Fluorophenyl)sulfonyl]methylamino]-1,2,3,4-tetrahydro-9H-carbazole-9-acetic acid
CAS627865-18-3
MFC21H21FN2O4S
MW416.47
EINECS
MOL File627865-18-3.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:5): 0.5 mg/ml; Ethanol: 15 mg/ml
form	A crystalline solid
color	White to off-white

Usage And Synthesis

Uses

CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model[1][2][3].

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.

IC 50

CRTH2

References

[1] Hatanaka M, et al. 15d-prostaglandin J2 enhancement of nerve growth factor-induced neurite outgrowth is blocked by the chemoattractant receptor- homologous molecule expressed on T-helper type 2 cells (CRTH2)antagonistCAY10471 in PC12 cells. J Pharmacol Sci.2010;113(1):89-93. Epub 2010 Apr 16. DOI:10.1254/jphs.10001sc
[2] Matsushima Y, et al. Distinct roles of prostaglandin D2 receptors in chronic skin inflammation.Mol Immunol. 2011 Oct;49(1-2):304-10. DOI:10.1016/j.molimm.2011.08.023
[3] Ito H, et al. PGD2-CRTH2pathway promotes tubulointerstitial fibrosis.J Am Soc Nephrol.2012 Nov;23(11):1797-809. DOI:10.1681/ASN.2012020126

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