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Cat. No.: HY-137107

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Radafaxine

(Synonyms: (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.

For research use only. We do not sell to patients.

CAS No.: 192374-14-4
Formula: C₁₃H₁₈ClNO₂
Molecular Weight:255.74

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

Data Sheet (268 KB)

Radafaxine Chemical Structure

CAS No.: 192374-14-4

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Fluorescent Dye

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

Biological Activity
- Description
- Cellular Effect
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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]

Chemical Information

CAS No. 192374-14-4
Molecular Weight 255.74
Formula C₁₃H₁₈ClNO₂
SMILES

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

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (1)

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Journal Impact Factor

Nature

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

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

Purity & Documentation

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[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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Help & FAQs

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.

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Biological Activity
- Description
Chemical Information
Publications (1)
Purity & Documentation
References

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Radafaxine

Publications Citing Use of MedChemExpress (MCE) Radafaxine