3-Hydroxy agomelatine

SKU: orb2901847

Description

3-Hydroxy agomelatine is a metabolite of Agomelatine. 3-Hydroxy agomelatine is a 5-HT2C receptor antagonist with an IC50 of 3.2 μM and a Ki of 1.8 μM.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	166526-99-4
MW	259.3
Purity	>98% (HPLC)
Formula	C₁₅H₁₇NO₃
SMILES	COc1ccc2cc(O)cc(CCNC(C)=O)c2c1
Target	5-HT Receptor
Solubility	In Vitro: DMSO : 250 mg/mL (964.13 mM; Ultrasonic )

Bioactivity

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In Vivo	Increasing doses (from 1.25 to 40 mg/kg, intraperitoneal injection) of 3-Hydroxy agomelatine (S 21540) does not affect the penile erections induced by mCPP and Ro 60-0175 in Wistar rat.
In Vitro	Agomelatine and S 21517 have moderately high affinities for 5-HT2C receptors (Ki = 0.21 μM and 0.13 μM, respectively). The metabolite 3-Hydroxy agomelatine (S 21540) has a 10-fold lower affinity (Ki = 1.8 μM). Agomelatine, S 21517 and 3-Hydroxy agomelatine (10-7-10-4 M) are antagonists at 5-HT2C receptors, with a rank order of efficacy as follows: S 21517>Agomelatine>3-Hydroxy agomelatine.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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Quick Database Links

Gene Symbol

5-HT Receptor

Protocol Information

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Purity:	100.00% (May vary between batches)
CAS Number:	166526-99-4
MW:	259.3
Formula:	C₁₅H₁₇NO₃

CAS Number:	1079774-23-4
MW:	262.32
Formula:	C₁₅H₁₇NO₃