| Identification | Back Directory | [Name]
5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE | [CAS]
158848-32-9 | [Synonyms]
GR 159897 5-Fluoro-3-[2-[4-methoxy-4-[[-phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole (R)-5-Fluoro-3-[2-[4-methoxy-4-[(phenylsulfinyl)methyl]-1-piperidinyl]ethyl]-1H-indole 5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1H-indole 5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE 1H-Indole, 5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]- | [Molecular Formula]
C23H27FN2O2S | [MDL Number]
MFCD05665140 | [MOL File]
158848-32-9.mol | [Molecular Weight]
414.54 |
| Chemical Properties | Back Directory | [Boiling point ]
600.2±55.0 °C(Predicted) | [density ]
1.29±0.1 g/cm3(Predicted) | [storage temp. ]
−20°C
| [solubility ]
DMSO: ~24 mg/mL, soluble
| [form ]
solid
| [pka]
16.46±0.30(Predicted) | [color ]
off-white
|
| Hazard Information | Back Directory | [Uses]
GR 159897 is an NK2 receptor antagonist which aids in the treatment of IBS. | [Biological Activity]
A potent, selective, non-peptide, orally active neurokinin NK 2 receptor antagonist. Competes for binding of [ 3 H]GR100679 to hNK 2 -transfected CHO cells with a pK i of 9.5. Inhibits NK 2 receptor-mediated contraction of guinea pig trachea with a pA 2 of 8.7. Anxiolytic in vivo . | [in vivo]
GR 159897 (0.12 mg/kg; intravenous injection; guinea-pigs) treatment potently antagonizes bronchoconstriction induced by GR64349, with a long duration of action (3 h)[1]. | Animal Model: | Guinea-pigs[1] | | Dosage: | 0.12 mg/kg | | Administration: | Intravenous injection | | Result: | Potently antagonised bronchoconstriction induced by GR64349, with a long duration of action (3 h).
|
| [IC 50]
NK2: 10 (pKi, Rat colon membrane); hNK2: 9.51 (pKi, CHO cell) | [storage]
Desiccate at -20°C |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Carbosynth
|
| Tel: |
+86 512 6260 5585 |
| Website: |
www.carbosynth.com |
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