| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
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| Targets |
F-15599 is a selective agonist at 5-HT1A receptors (Ki = 0.8 nM for rat 5-HT1A receptors). It shows >100-fold selectivity over 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, D1, D2, and α1-adrenoceptors. It exhibits biased agonism toward Gi protein signaling and preferentially activates postsynaptic 5-HT1A receptors. [3]
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| ln Vitro |
F-15599 (NLX-101) exhibited 100-fold selectivity for 5-HT1A over other serotonin receptor subtypes in radioligand binding assays [3].
Demonstrated biased agonism profile with preferential activation of Gαi/o over β-arrestin signaling pathways [2].
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| ln Vivo |
F-15599 (0.16 mg/kg s.c.) increased prefrontal cortex dopamine levels by 200% in rats, while reducing serotonin levels in the dorsal raphe nucleus, confirming preferential postsynaptic activity. This effect was blocked by the 5-HT1A antagonist WAY100635. [3]
In a rat model of aggression (resident-intruder test), F-15599 (0.04–0.63 mg/kg s.c.) significantly reduced attack duration and frequency at 0.16 mg/kg. These anti-aggressive effects were reversed by WAY100635, confirming 5-HT1A mediation. [2] F-15599 (0.0025–0.04 mg/kg i.v.) induced lower lip retraction and flat body posture in rats, but with 3-fold higher potency for postsynaptic responses (ED50 = 0.005 mg/kg) than presynaptic effects (ED50 = 0.016 mg/kg). [3] |
| Animal Protocol |
For aggression studies, F-15599 was dissolved in saline and administered subcutaneously (s.c.) at doses of 0.04, 0.16, and 0.63 mg/kg 30 minutes before behavioral testing. Control groups received saline. [2]
For neurochemical and behavioral assays, F-15599 was injected intravenously (i.v.) at 0.0025–0.04 mg/kg or subcutaneously at 0.16 mg/kg. WAY100635 (0.16 mg/kg s.c.) was administered 20 minutes prior to F-15599 for antagonism tests. [3] |
| References |
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| Additional Infomation |
F-15599 is a high-efficacy "biased agonist" that preferentially targets cortical postsynaptic 5-HT1A receptors over somatodendritic autoreceptors, enhancing frontal cortex dopamine release. This contrasts with classical 5-HT1A agonists like 8-OH-DPAT. [3]
Its anti-aggressive effects are mediated via postsynaptic 5-HT1A receptors in corticolimbic regions, suggesting therapeutic potential for impulse control disorders. [2] |
| Molecular Formula |
C26H29CLF2N4O4S
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|---|---|
| Molecular Weight |
567.047671079636
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| Exact Mass |
566.156610
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| Elemental Analysis |
C, 55.07; H, 5.16; Cl, 6.25; F, 6.70; N, 9.88; O, 11.29; S, 5.65
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| CAS # |
955112-72-8
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| Related CAS # |
635323-95-4; 955112-72-8; 635323-96-5 (fumarate)
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| PubChem CID |
23626316
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
ClC1=C(C=CC(=C1)C(N1CCC(CNCC2N=CC(C)=CN=2)(CC1)F)=O)F.S(C1C=CC(C)=CC=1)(=O)(=O)O
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| Synonyms |
NLX-101 tosylate; F-15599 Tosylate; NLX-101 tosylate; F-15,599 Tosylate; 955112-72-8; 35513476QO; UNII-35513476QO; Methanone, (3-chloro-4-fluorophenyl)(4-fluoro-4-((((5-methyl-2-pyrimidinyl)methyl)amino)methyl)-1-piperidinyl)-, 4-methylbenzenesulfonate (1:1)
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7635 mL | 8.8176 mL | 17.6351 mL | |
| 5 mM | 0.3527 mL | 1.7635 mL | 3.5270 mL | |
| 10 mM | 0.1764 mL | 0.8818 mL | 1.7635 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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