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Merck

SML2743

Sigma-Aldrich

TM30089

≥98% (HPLC)

别名:

2-(3-(4-Fluoro-N-methylphenylsulfonamido)-3,4-dihydro-1H-carbazol-9(2H)-yl)acetic acid, 3-[[(4-Fluorophenyl)sulfonyl]methylamino]-1,2,3,4-tetrahydro-9H-carbazole-9-acetic acid, CAY 10471, CAY-10471, CAY10471, TM 30089, TM-30089, {3-[(4-Fluorobenzenesulfonyl)methylamino]-1,2,3,4-tetrahydrocarbazol-9-yl}acetic acid

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About This Item

经验公式(希尔记法):
C21H21FN2O4S
分子量:
416.47
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

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)

InChI 密鑰

CANCTKXGRVNXFP-UHFFFAOYSA-N

生化/生理作用

TM30089 is a ramatroban analog and an orally active, high-affinity, potent and selective prostaglandin D2 receptor 2 (DP2; CRTH2) antagonist (Ki = 0.6 nM/hDP2 against 1.2 nM PGD2; Ki = 1.2 μM/hDP1 against 0.5 nM PGD2, >10 μM/hTP against 5 nM SQ29548) that blocks PGD2-induced responses in hDP2 transfectants (IP1/βarr IC50 = 1.2/3.0 nM) and exhibits in vivo efficacy in a murine model of renal tubulointerstitial fibrosis (20 mg/kg b.i.d. p.o., starting 4 days before or 3 days after unilateral ureteral obstruction/UUO).

象形圖

Exclamation markEnvironment

訊號詞

Warning

危險分類

Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Skin Irrit. 2 - Skin Sens. 1

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3


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Trond Ulven et al.
Journal of medicinal chemistry, 48(4), 897-900 (2005-02-18)
Ramatroban, a thromboxane A(2) receptor (TP) antagonist with clinical efficacy in asthma and allergic rhinitis, was recently shown to also antagonize the prostaglandin D(2) receptor CRTH2. Here we report that minor structural changes to ramatroban result in a compound (13)
Go Eun Choi et al.
The Journal of allergy and clinical immunology, 141(3), 938-950 (2017-12-12)
Eosinophilic inflammation is a major pathologic feature of chronic rhinosinusitis (CRS) and is frequently associated with severe refractory disease. Prostaglandin (PG) D2 levels are increased in patients with CRS, and PGD2 is an important contributing factor to eosinophilic inflammation. Autophagy
Hideyuki Ito et al.
Journal of the American Society of Nephrology : JASN, 23(11), 1797-1809 (2012-09-22)
Urinary excretion of lipocalin-type PGD(2) synthase (L-PGDS), which converts PG H(2) to PGD(2), increases in early diabetic nephropathy. In addition, L-PGDS expression in the tubular epithelium increases in adriamycin-induced nephropathy, suggesting that locally produced L-PGDS may promote the development of
Miriam Peinhaupt et al.
Journal of leukocyte biology, 104(1), 159-171 (2018-04-03)
Prostaglandin (PG) D2 is the ligand for the G-protein coupled receptors DP1 (D-type prostanoid receptor 1) and DP2 (also known as chemoattractant receptor homologous molecule, expressed on Th2 cells; CRTH2). Both, DP1 and DP2 are expressed on the cellular surface
David F Woodward et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 31(1), 368-375 (2016-10-23)
The purpose of these studies was to test the hypothesis that a selected polypharmacological approach for treating the prostanoid-mediated component of inflammatory diseases would produce a therapeutic effect superior to global inhibition of prostaglandin (PG) biosynthesis by aspirin-like drugs. The

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