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Asenapine

🥰Excellent
Catalog No. T21360Cas No. 65576-45-6
Alias Org 5222, ME2136, HSDB 8061

Asenapine (Org 5222) is a 5-HT receptor, adrenergic receptor, dopamine receptor, and histamine receptor antagonist with antipsychotic effects that is used to treat schizophrenia and manic or mixed episodes associated with bipolar 1 disorder.721483-46-5

Asenapine

Asenapine

🥰Excellent
Purity: 99.16%
Catalog No. T21360Alias Org 5222, ME2136, HSDB 8061Cas No. 65576-45-6
Asenapine (Org 5222) is a 5-HT receptor, adrenergic receptor, dopamine receptor, and histamine receptor antagonist with antipsychotic effects that is used to treat schizophrenia and manic or mixed episodes associated with bipolar 1 disorder.721483-46-5
Pack SizePriceAvailabilityQuantity
1 mg$32In Stock
5 mg$72In Stock
10 mg$98In Stock
25 mg$168In Stock
50 mg$247In Stock
100 mg$365In Stock
1 mL x 10 mM (in DMSO)$80In Stock
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Purity:99.16%
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Product Introduction

Bioactivity
Description
Asenapine (Org 5222) is a 5-HT receptor, adrenergic receptor, dopamine receptor, and histamine receptor antagonist with antipsychotic effects that is used to treat schizophrenia and manic or mixed episodes associated with bipolar 1 disorder.721483-46-5
Targets&IC50
5-HT1A receptor:8.6 (pKi), 5-HT2A receptor:10.2 (pKi), 5-HT1B receptor:8.4 (pKi), 5-HT2B receptor:9.8 (pKi)
In vitro
In comparison with the antipsychotics, asenapine showed high affinity and a different rank order of binding affinities (pKi) for serotonin receptors (5-HT1A [8.6], 5-HT1B [8.4], 5-HT2A [10.2], 5-HT2B [9.8], 5-HT2C [10.5], 5-HT5 [8.8], 5-HT6 [9.6] and 5-HT7 [9.9]), adrenoceptors (alpha1 [8.9], alpha2A [8.9], alpha2B [9.5] and alpha2C [8.9]), dopamine receptors (D1 [8.9], D2 [8.9], D3 [9.4] and D4 [9.0]) and histamine receptors (H1 [9.0] and H2 [8.2])[2].
In vivo
Asenapine (0.05-0.2 mg/kg, s.c.) induced a dose-dependent suppression of CAR (no escape failures recorded) and did not induce catalepsy. Additionally, it increased dopamine efflux in both the medial prefrontal cortex (mPFC) and the nucleus accumbens (NAc)[2].
AliasOrg 5222, ME2136, HSDB 8061
Chemical Properties
Molecular Weight285.77
FormulaC17H16ClNO
Cas No.65576-45-6
Smiles[H][C@@]12CN(C)C[C@@]1([H])c1cc(Cl)ccc1Oc1ccccc21
Relative Density.1.231
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: Insoluble
DMSO: 80 mg/mL (279.94 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.4993 mL17.4966 mL34.9932 mL174.9659 mL
5 mM0.6999 mL3.4993 mL6.9986 mL34.9932 mL
10 mM0.3499 mL1.7497 mL3.4993 mL17.4966 mL
20 mM0.1750 mL0.8748 mL1.7497 mL8.7483 mL
50 mM0.0700 mL0.3499 mL0.6999 mL3.4993 mL
100 mM0.0350 mL0.1750 mL0.3499 mL1.7497 mL

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