Art. -Nr.: HY-19863

F-15599

Name: F-15599
Brand: MedChemExpress
SKU: HY-19863
Price: 125.00 USD
Availability: InStock
Rating: 5 (2 reviews)

(Synonyms: NLX-101)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.

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Reinheit : 99.13%
CAS. Nr.: 635323-95-4
Formel: C₁₉H₂₁ClF₂N₄O
Molecular Weight:394.85

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

F-15599 Chemical Structure

CAS. Nr.: 635323-95-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.

IC₅₀ & Target

5-HT_1A Receptor

3.4 nM (Ki)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

In Vivo

F15599 (0.06 or 0.12 mg/kg) significantly reduces l-DOPA-induced dyskinesia (LID), without affecting motor performance of rats. Rats treated with F15599 manifest less LID and mild 5-HT syndrome with the high dose of 30 μg/μL^[1]. F15599 (0.0625, 0.125, 0.25, 0.5 and 1.0 mg/kg, i,p,) results in a significant and dose-dependent (MED = 0.125 mg/kg) delay in the latency to attack, and a potent reduction (ID₅₀ = 0.095 mg/kg) in the amount of aggressive behaviour directed towards the intruder rat. Starting from the 0.25 mg/kg dose, F15599 induces clear signs of the so-called serotonin syndrome characterized by flat body posture, head-waving, lower lip retraction and hindlimb abduction, leading to increased behavioural inactivity scores and social disengagement^[2]. F15599 increases the discharge rate of pyramidal neurones in medial prefrontal cortex (mPFC) from 0.2 μg/kg i.v and reduces that of dorsal raphe 5-hydroxytryptaminergic neurones at doses >10-fold higher (minimal effective dose 8.2 μg/kg i.v.). F15599 increases dopamine output in mPFC (an effect dependent on the activation of postsynaptic 5-HT1A receptors) with an ED₅₀ of 30 μg/kg i.p., whereas it reduces hippocampal 5-HT release (an effect dependent exclusively on 5-HT1A autoreceptor activation) with an ED₅₀ of 240 μg/kg i.p^[3].

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

Chemical Information

CAS. Nr. 635323-95-4
Appearance Solid
Molecular Weight 394.85
Formel C₁₉H₂₁ClF₂N₄O
Color White to off-white
SMILES

O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CNCC3=NC=C(C)C=N3)(F)CC2
Synonyms

NLX-101
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (2)

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Journal Impact Factor

Mol Pharmacol

G α Protein Signaling Bias at Serotonin 1A Receptor. [Abstract]

2023 Nov;104(5):230-238. PMID: 37567783
Pharmacol Biochem Behav

Prevention of MK-801-induced amnestic effect with combined activation of 5-HT1A and muscarinic receptors in mice. [Abstract]

2024 May:238:173749. PMID: 38462045

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (633.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5326 mL

12.6630 mL

25.3261 mL

5 mM

0.5065 mL

2.5326 mL

5.0652 mL

10 mM

0.2533 mL

1.2663 mL

2.5326 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.17 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.17 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.17 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[2]

Briefly, in this paradigm, male rats are housed individually in large observation cages (80 × 55 × 50 cm) with an oviduct-ligated female to avoid social isolation and allow sexual behaviour, thereby facilitating territorial behaviour. After 1 week, the baseline level of offensive aggressive behaviour is tested on 3 consecutive days during maximally a 10-min confrontation with an unfamiliar male conspecific (WTG rats). The female partner of the experimental rat is removed from the home observation cage approximately 60 min prior to the start of this social provocation test. Naive male WTG rats, socially housed in groups of 3 in transparent makrolon type IV cages, are used as conspecific intruder animals (average weight 372 ± 9.5 g and 3.5-4 months old). During the first 3 tests, the intruder is removed immediately after the first full attack from the resident and the attack latency time (ALT) is noted. Experimental groups are balanced on the basis of the ALT and the level of offensive behaviour performed during the fourth baseline test (day 4), during which the full range of behaviours is recorded and analysed. Only animals that attacked (i.e. ALT <600 s) are included in the experimental groups. Non-attacking individuals (11 out of 144) are excluded from this study. On the next day (day 5), vehicle (sterile Ultra Pure water, n = 19 and n = 20) or either F15599 (0.0625, 0.125, 0.25, 0.5 and 1.0 mg/kg, IP, experiment 1, n = 45) or F13714 (0.003, 0.006, 0.012, 0.025, 0.062, 0.125, 0.250, IP, experiment 2, n = 50) is administered 30 min before the 10 min confrontation with a drug-free unfamiliar intruder conspecific and their behaviour is recorded again. In addition, in experiment 3, animals are tested 30 min after treatment with either vehicle/vehicle (UP), vehicle/F15599 (0.1 mg/kg) or F13714, WAY-100635 (0.3 mg/kg)/vehicle or WAY100635 (0.3 mg/kg)/ F15599 (0.1 mg/kg) or F13714. Each treatment group consists of 6-8 subjects (n = 41 animals total).

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[1]. Meadows SM, et al. Characterizing the differential roles of striatal 5-HT1A auto- and hetero-receptors in the reduction of l-DOPA-induced dyskinesia. Exp Neurol. 2017 Jun;292:168-178. [Content Brief]

[2]. de Boer SF, et al. Anti-aggressive effects of the selective high-efficacy 'biased' 5-HT?A receptor agonists F15599 and F13714 in male WTG rats. Psychopharmacology (Berl). 2016 Mar;233(6):937-47. [Content Brief]

[3]. Lladó-Pelfort L, et al. Preferential in vivo action of F15599, a novel 5-HT(1A) receptor agonist, at postsynaptic 5-HT(1A) receptors. Br J Pharmacol. 2010 Aug;160(8):1929-40. [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5326 mL	12.6630 mL	25.3261 mL	63.3152 mL
	5 mM	0.5065 mL	2.5326 mL	5.0652 mL	12.6630 mL
	10 mM	0.2533 mL	1.2663 mL	2.5326 mL	6.3315 mL
	15 mM	0.1688 mL	0.8442 mL	1.6884 mL	4.2210 mL
	20 mM	0.1266 mL	0.6332 mL	1.2663 mL	3.1658 mL
	25 mM	0.1013 mL	0.5065 mL	1.0130 mL	2.5326 mL
	30 mM	0.0844 mL	0.4221 mL	0.8442 mL	2.1105 mL
	40 mM	0.0633 mL	0.3166 mL	0.6332 mL	1.5829 mL
	50 mM	0.0507 mL	0.2533 mL	0.5065 mL	1.2663 mL
	60 mM	0.0422 mL	0.2111 mL	0.4221 mL	1.0553 mL
	80 mM	0.0317 mL	0.1583 mL	0.3166 mL	0.7914 mL
	100 mM	0.0253 mL	0.1266 mL	0.2533 mL	0.6332 mL

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Keywords

F-15599

2 Cited Publications

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F-15599

Publications Citing Use of MedChemExpress (MCE) F-15599

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