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製品番号: HY-137107

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Radafaxine

(別名: (S,S)-Hydroxybupropion; GW-353162A free base; BW-306U free base)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Radafaxine ((S,S)-Hydroxybupropion) is an antidepressant. Radafaxine blocks dopamine transporters (DAT). Radafaxine is an active metabolite of Bupropion.

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CAS 番号: 192374-14-4
分子式: C₁₃H₁₈ClNO₂
分子量:255.74

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

Radafaxine 構造式

CAS 番号: 192374-14-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

Radafaxine ((S,S)-Hydroxybupropion) is an antidepressant. Radafaxine blocks dopamine transporters (DAT). Radafaxine is an active metabolite of Bupropion^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>100 μM Compound: (2S,3S)-4a	Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells after 90 mins by scintillation counting Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells after 90 mins by scintillation counting	[PMID: 20509659]
HEK293	IC₅₀	>100 μM Compound: (2S,3S)-4a	Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells after 90 mins by scintillation counting Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells after 90 mins by scintillation counting	[PMID: 20509659]
HEK293	IC₅₀	100 nM Compound: (S,S)-5a	Inhibition of human NET in HEK293 cells assessed as inhibition of [3H]norepinephrine uptake Inhibition of human NET in HEK293 cells assessed as inhibition of [3H]norepinephrine uptake	[PMID: 21319801]
HEK293	IC₅₀	20 μM Compound: (S,S)-5a	Antagonist activity at human alpha4beta2 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux Antagonist activity at human alpha4beta2 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux	[PMID: 21319801]
HEK293	IC₅₀	220 nM Compound: (S,S)-5a	Inhibition of human DAT in HEK293 cells assessed as inhibition of [3H]dopamine uptake Inhibition of human DAT in HEK293 cells assessed as inhibition of [3H]dopamine uptake	[PMID: 21319801]
HEK293	IC₅₀	3.3 μM Compound: (S,S)-5a	Antagonist activity at human alpha3beta4 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux Antagonist activity at human alpha3beta4 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux	[PMID: 21319801]
HEK293	IC₅₀	30 μM Compound: (S,S)-5a	Antagonist activity at human alpha4beta4 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux Antagonist activity at human alpha4beta4 nAChR in HEK293 cells assessed as inhibition of carbamylcholine-induced radiolabeled Rb ion efflux	[PMID: 21319801]
HEK293	IC₅₀	387 nM Compound: (S,S)-5a	Inhibition of human SERT in HEK293 cells assessed as inhibition of [3H]serotonin uptake Inhibition of human SERT in HEK293 cells assessed as inhibition of [3H]serotonin uptake	[PMID: 21319801]
HEK293	IC₅₀	9900 nM Compound: (2S,3S)-4a	Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells after 90 mins by scintillation counting Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells after 90 mins by scintillation counting	[PMID: 20509659]
SH-SY5Y	IC₅₀	6.5 μM Compound: (2S,3S)-4a	Antagonist activity at alpha3beta4 nicotinic receptor in human SH-SY5Y cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting Antagonist activity at alpha3beta4 nicotinic receptor in human SH-SY5Y cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting	[PMID: 20509659]
TE-671	IC₅₀	7.6 μM Compound: (2S,3S)-4a	Antagonist activity at alpha-1-beta-1-gamma-delta nicotinic receptor in human TE671 cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting Antagonist activity at alpha-1-beta-1-gamma-delta nicotinic receptor in human TE671 cells assessed as inhibition varbamylcholine-induced radiolabeled Rb+ influx at by liquid scintillation counting	[PMID: 20509659]

化学情報

CAS 番号 192374-14-4
分子量 255.74
分子式 C₁₃H₁₈ClNO₂
SMILES

O[C@]1(C2=CC=CC(Cl)=C2)[C@H](C)NC(C)(C)CO1
別名

(S,S)-Hydroxybupropion; GW-353162A free base; BW-306U free base
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Nature

Substrate binding and inhibition mechanism of norepinephrine transporter. [Abstract]

2024 Sep;633(8029):473-479. PMID: 39143211

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (268 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Volkow ND, et al. The slow and long-lasting blockade of dopamine transporters in human brain induced by the new antidepressant drug radafaxine predict poor reinforcing effects. Biol Psychiatry. 2005 Mar 15;57(6):640-6. [Content Brief]

[2]. Xu H, et al. Stereoselective analysis of hydroxybupropion and application to drug interaction studies. Chirality. 2007 Mar;19(3):163-70. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Radafaxine

1 Cited Publications

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化学情報
Publications (1)
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Radafaxine

MedChemExpress（MCE）の使用を引用している文献 Radafaxine

生物活性

化学情報

Publications (1)

純度とドキュメンテーション

参考文献

Calculators

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Radafaxine 関連分類

HY-137107 関連分類