627865-18-3

627865-18-3 structure

Name: CAY10471
Chemical Name: 2-[3-[(4-fluorophenyl)sulfonylmethylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]acetic acid
CAS Number: 627865-18-3
Molecular Formula: C₂₁H₂₁FN₂O₄S
Molecular Weight: 416.466
Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
Create Date: 2017-03-10 10:24:29
Modify Date: 2024-01-10 17:27:27
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].

Name	2-[3-[(4-fluorophenyl)sulfonylmethylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]acetic acid
Synonyms	9H-Carbazole-9-propanoic acid, 3-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro- 3-(3-{[(4-Fluorophenyl)sulfonyl]amino}-1,2,3,4-tetrahydro-9H-carbazol-9-yl)propanoic acid

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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor Research Areas >> Inflammation/Immunology
Target	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.
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) antagonist CAY10471 in PC12 cells. J Pharmacol Sci. 2010;113(1):89-93. Epub 2010 Apr 16. [2]. Matsushima Y, et al. Distinct roles of prostaglandin D2 receptors in chronic skin inflammation.Mol Immunol. 2011 Oct;49(1-2):304-10. [3]. Ito H, et al. PGD2-CRTH2 pathway promotes tubulointerstitial fibrosis.J Am Soc Nephrol. 2012 Nov;23(11):1797-809.

Density	1.4±0.1 g/cm3
Boiling Point	654.7±65.0 °C at 760 mmHg
Molecular Formula	C₂₁H₂₁FN₂O₄S
Molecular Weight	416.466
Flash Point	349.7±34.3 °C
Exact Mass	416.120605
PSA	87.99000
LogP	4.09
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.664

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