1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. NLX-204 hydrochloride

NLX-204 hydrochloride 

Cat. No.: HY-124631A
Handling Instructions

NLX-204 (hydrochloride) is an orally active, potent, highly affinity and selective 5-HT1A receptor-biased agonist (pKi=10.19). NLX-204 (hydrochloride) shows relatively higher affinity for α1 and D2 receptors than for other off-targets. NLX-204 (hydrochloride) can be used for the research of antidepressant.

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

NLX-204 hydrochloride Chemical Structure

NLX-204 hydrochloride Chemical Structure

Size Price Stock Quantity
5 mg USD 170 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 460 In-stock
Estimated Time of Arrival: December 31
50 mg USD 650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 980 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of NLX-204 hydrochloride:

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Description

NLX-204 (hydrochloride) is an orally active, potent, highly affinity and selective 5-HT1A receptor-biased agonist (pKi=10.19). NLX-204 (hydrochloride) shows relatively higher affinity for α1 and D2 receptors than for other off-targets. NLX-204 (hydrochloride) can be used for the research of antidepressant[1].

IC50 & Target[1]

5-HT1A Receptor

10.19 (pKi)

In Vitro

NLX-204 (10 μM) (hydrochloride) shows substantial binding inhibition (higher than 50%) for adrenergic α1A and α2A and dopaminergic D2S receptors. NLX-204 (1 μM) (hydrochloride) exhibits much lower binding inhibition at D2 and α2A receptors but maintains a relatively high value for the α1Areceptor. NLX-204 (0.1~10 μM) (hydrochloride) has a low propensity for hERG channel blockade and suggests that the investigated series has a low risk with respect to hERG-related cardiac safety. NLX-204 (hydrochloride) also exhibits high microsomal stability. NLX-204 (hydrochloride) displays no P-gp inhibition (6.5% of inhibition at 10 μM) as well as negligible inhibition of CYP3A4 and CYP2D6 (23.2 and 15.9% at 10 μM, respectively). NLX-204 (hydrochloride) does not elicit flat body posture (FBP), a common side effect of the 5-HT1A receptor stimulation, suggesting that its preference for activation of 5-HT1A receptor-mediated ERK1/2 phosphorylation in vitro translates to preferential antidepressant effects rather than induction of "behavioral syndrome"[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NLX-204 (2.5 mg/kg; p.o.) (hydrochloride) is rapidly absorbed from the gastrointestinal tract (Tmax = 15 min), reaches relatively high serum concentrations and shows higher concentration than those in serum for all doses[1].
NLX-204 (0.04~2.5 mg/kg; p.o.) (hydrochloride) shows that statistically significant elevation of pERK1/2 is observed at the two highest doses (2.5 and 0.63 mg/kg), but a tendency to increase pERK1/2 levels is also seen at lower doses[1].
NLX-204 (hydrochloride) robustly and significantly increases rat PFC ERK1/2 phosphorylation in a time dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (170~200 g)[1]
Dosage: 2.5 mg/kg
Administration: P.o.
Result: Rapidly absorbed from the gastrointestinal tract (Tmax = 15 min) and reached relatively high serum concentrations.
Animal Model: Male Wistar rats (170~200 g)[1]
Dosage: 2.5 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: The concentration of NLX-204 in brain tissue was higher than those in serum for all doses.
Animal Model: Male Wistar rats (170~200 g)[1]
Dosage: 0.04~2.5 mg/kg
Administration: P.o.
Result: Statistically significant elevation of pERK1/2 was observed at the two highest doses (2.5 and 0.63 mg/kg), but a tendency to increase pERK1/2 levels was also seen at lower doses.
Molecular Weight

446.32

Formula

C₂₀H₂₃Cl₂F₂N₃O₂

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (224.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2405 mL 11.2027 mL 22.4054 mL
5 mM 0.4481 mL 2.2405 mL 4.4811 mL
10 mM 0.2241 mL 1.1203 mL 2.2405 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
NLX-204 hydrochloride
Cat. No.:
HY-124631A
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