Product Name :
Lusaperidone
Description:
Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
CAS:
214548-46-6
Molecular Weight:
359.42
Formula:
C22H21N3O2
Chemical Name:
2-methyl-3-(2-8-oxa-4-azatricyclo[7.4.0.0²,⁷]trideca-1(13),2(7),9,11-tetraen-4-ylethyl)-4H-pyrido[1,2-a]pyrimidin-4-one
Smiles :
CC1N=C2C=CC=CN2C(=O)C=1CCN1CC2C3=CC=CC=C3OC=2CC1
InChiKey:
ZYXHQIPQIKTEDI-UHFFFAOYSA-N
InChi :
InChI=1S/C22H21N3O2/c1-15-16(22(26)25-11-5-4-8-21(25)23-15)9-12-24-13-10-20-18(14-24)17-6-2-3-7-19(17)27-20/h2-8,11H,9-10,12-14H2,1H3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.|Product information|CAS Number: 214548-46-6|Molecular Weight: 359.42|Formula: C22H21N3O2|Chemical Name: 2-methyl-3-(2-8-oxa-4-azatricyclo[7.4.0.0²,⁷]trideca-1(13),2(7),9,11-tetraen-4-ylethyl)-4H-pyrido[1,2-a]pyrimidin-4-one|Smiles: CC1N=C2C=CC=CN2C(=O)C=1CCN1CC2C3=CC=CC=C3OC=2CC1|InChiKey: ZYXHQIPQIKTEDI-UHFFFAOYSA-N|InChi: InChI=1S/C22H21N3O2/c1-15-16(22(26)25-11-5-4-8-21(25)23-15)9-12-24-13-10-20-18(14-24)17-6-2-3-7-19(17)27-20/h2-8,11H,9-10,12-14H2,1H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.Nebivolol manufacturer |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.C18-Ceramide custom synthesis |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Lusaperidone has subnanomolar affinity for α2A and α2C adrenergic receptor (Ki=0.PMID:32985927 13 and 0.15 nM, respectively) and shows nanomolar affinity for the hα2B adrenergic receptor and h5-HT7 receptors (Ki=1 and 5 nM, respectively). Lusaperidone interacts weakly (Ki values ranging between 81 and 920 nM) with dopamine-hD2L, -hD3 and -hD4, h5-HT1D-, h5-HT1F-, h5-HT2A-, h5-HT2C-, and h5-HT5A receptors. Lusaperidone, tested up to 10 μM, interacts only at micromolar concentrations or not at all with any of the other receptor or transporter binding sites tested in this study. Lusaperidone has been shown to reverse the clonidine-induced inhibition of cyclic AMP production mediated by human α2A and α2C adrenoceptors expressed in cell lines (Kb is 2.8 and 4.4 nM, respectively) and is a full antagonist on both receptor subtypes.|In Vivo:|Lusaperidone occupies the α2A and α2C adrenergic receptor with an ED50 of 0.014 mg/kg sc (0.009-0.019) and 0.026 mg/kg sc (0.022-0.030), respectively. The uptake of R107474 after in vivo intravenous administration is very rapid; in most tissues (including the brain) it reaches maximum concentration at 5 min after tracer injection.|Products are for research use only. Not for human use.|