(+)-3-[[(4-FLUOROPHENYL)SULFONYL]METHYLAMINO]-1,2,3,4-TETRAHYDRO-9H-CARBAZOLE-9-ACETIC ACID Chemical Properties

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

(+)-3-[[(4-FLUOROPHENYL)SULFONYL]METHYLAMINO]-1,2,3,4-TETRAHYDRO-9H-CARBAZOLE-9-ACETIC ACID Usage And Synthesis

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 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) 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)

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

(+)-3-[[(4-FLUOROPHENYL)SULFONYL]METHYLAMINO]-1,2,3,4-TETRAHYDRO-9H-CARBAZOLE-9-ACETIC ACID(844639-57-2)Related Product Information

• TPP
• 4'-Hydroxyacetophenone
• 2-FLUOROPHENYL CYCLOPENTYL KETONE
• TRIS(PENTAFLUOROPHENYL)BORANE
• Aniline