| Identification | Back Directory | [Name]
(+)-3-[[(4-FLUOROPHENYL)SULFONYL]METHYLAMINO]-1,2,3,4-TETRAHYDRO-9H-CARBAZOLE-9-ACETIC ACID | [CAS]
844639-57-2 | [Synonyms]
TM30089
CS-1157
TM30089 Racemate
TM 30089;TM-30089
CAY10471 Racemate
TM30089 (CAY10471)
9H-Carbazole-9-acetic acid, 3-[[(4-fluorophenyl)sulfonyl]MethylaMino]-1,2,3,4-tetrahydro-
(+)-3-[[(4-FLUOROPHENYL)SULFONYL]METHYLAMINO]-1,2,3,4-TETRAHYDRO-9H-CARBAZOLE-9-ACETIC ACID | [Molecular Formula]
C21H21FN2O4S | [MDL Number]
MFCD08062186 | [MOL File]
844639-57-2.mol | [Molecular Weight]
416.47 |
| Chemical Properties | Back Directory | [Melting point ]
165-173℃ (dichloromethane ) | [Boiling point ]
639.1±65.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 150 mg/mL (360.17 mM) | [form ]
Solid | [pka]
4.33±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2[1]. | [Biological Activity]
TM30089 is a ramatroban analog and an orally activehigh-affinitypotent 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) th at 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). | [IC 50]
CRTH2: 0.6 nM (Ki) | [storage]
Store at -20°C | [References]
[1] Ulven T, et al. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem. 2005 Feb 24;48(4):897-900. DOI:10.1021/jm049036i |
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| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
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