(R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate manufacturers
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| | (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate Basic information | | Uses |
| Product Name: | (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate | | Synonyms: | (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate;BAY 38-7271;KN 38-7271;O-1861 (R-form);BAY-38-7071;1-Butanesulfonic acid, 4,4,4-trifluoro-,3-[[(2R)-2,3-dihydro-2-(hydroxyMethyl)-1H-inden-4-yl]oxy]phenyl ester;4,4,4-Trifluoro-1-butanesulfonic acid 3-[[(2R)-2,3-dihydro-2-(hydroxymethyl)-1H-inden-4-yl]oxy]phenyl ester;(R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate USP/EP/BP | | CAS: | 212188-60-8 | | MF: | C20H21F3O5S | | MW: | 430.4379496 | | EINECS: | | | Product Categories: | Pharmaceutical intermediate | | Mol File: | 212188-60-8.mol |  |
| | (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate Chemical Properties |
| Boiling point | 527.2±50.0 °C(Predicted) | | density | 1.350±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | pka | 14.81±0.10(Predicted) |
| | (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate Usage And Synthesis |
| Uses | Originally synthesized by chemist Wayne E. Kenney, BAY 38-7271 (KN 38-7271) is a drug which is a cannabinoid receptor agonist developed by Bayer AG. It has analgesic and neuroprotective effects and is used in scientific research, with proposed uses in the treatment of traumatic brain injury. It is a full agonist with around the same potency as CP 55,940 in animal studies, and has fairly high affinity for both CB1 and CB2 receptors, with Ki values of 2.91nM at CB1 and 4.24nM at CB2. It has been licensed to KeyNeurotek Pharmaceuticals for clinical development, and was in Phase II trials in 2008[6] but its development appears to have stopped. | | Uses | BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties[1]. | | in vivo | BAY 38-7271 (Ed50 = 0.02 mg/kg; i.v. and 0.5 mg/kg; i.p.) induces a potent and dose-de-pendent reduction in core body temperature[1].
BAY 38-7271 has low physical dependence liability and is not essentially different from that of other cannabinoid CB1 receptor agonists[1].
BAY 38-7271 (1-1000 ng/kg/h; i.v. infusion; for 4 hours) shows neuroprotective efficacy in the rat SDH model[1].
BAY 38-7271 also has neuroprotective efficacy in models of transient and permanent occlusion of the middle cerebral artery and brain edema models[1].
| Animal Model: | Wistar rat ,TBI rat models (acute subdural hematoma, SDH)[1] | | Dosage: | 1 ng/kg/h, 10 ng/kg/h, 100 ng/kg/h, 1000 ng/kg/h | | Administration: | Intravenous infusion, for 4 hours | | Result: | Reduced the mean infarct volume. |
| | IC 50 | CB1: 1.85 nM (Ki); CB2: 5.96 nM (Ki) | | References | [1] Mauler F, et al. BAY 38-7271: a novel highly selective and highly potent cannabinoid receptor agonist for the treatment of traumatic brain injury. CNS Drug Rev. 2003 Winter;9(4):343-58. DOI:10.1111/j.1527-3458.2003.tb00259.x |
| | (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate Preparation Products And Raw materials |
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