WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H532353
CAS#: 635323-95-4 (free base)
Description: NLX-101, also known as F-15,599, is a novel compound that activates serotonin 5-HT1A receptors with exceptional selectivity, having over 1000-fold higher affinity for this target over other receptors. In addition, NLX-101 is a 'biased agonist' at 5-HT1A receptors, preferentially activating 5-HT1A receptors in those brain regions that control mood and cognition.
Hodoodo Cat#: H532353
Name: NLX-101
CAS#: 635323-95-4 (free base)
Chemical Formula: C19H21ClF2N4O
Exact Mass: 394.14
Molecular Weight: 394.850
Elemental Analysis: C, 57.80; H, 5.36; Cl, 8.98; F, 9.62; N, 14.19; O, 4.05
Related CAS #: 635323-95-4 (free base) 955112-72-8 (tosylate) 635323-96-5 (fumarate)
Synonym: NLX-101; NLX 101; NLX101; F-15,599; F 15,599; F15,599; F15599; F-15599; F 15599;
IUPAC/Chemical Name: (3-Chloro-4-fluorophenyl)-[4-fluoro-4-[[(5-methylpyrimidin-2-ylmethyl)amino]methyl]piperidin-1-yl]methanone
InChi Key: O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CNCC3=NC=C(C)C=N3)(F)CC2
InChi Code: InChI=1S/C19H21ClF2N4O/c1-13-9-24-17(25-10-13)11-23-12-19(22)4-6-26(7-5-19)18(27)14-2-3-16(21)15(20)8-14/h2-3,8-10,23H,4-7,11-12H2,1H3
SMILES Code: O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CNCC3=NC=C(C)C=N3)(F)CC2
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | NLX-101, also known as F-15,599, is a novel compound that activates serotonin 5-HT1A receptors. |
| In vitro activity: | |
| In vivo activity: | The ability of NLX-101 to produce antidepressant-like activity was assessed in the FST following in-situ PFC unilateral microinjection. (+)8-OH-DPAT and F13714, two 5-HT1A receptor agonists that do not display cortical biased agonism, were tested as comparators. NLX-101 decreased time spent in immobility in a bi-modal manner, with a first MED of 0.25 μg (immobility reduced from 160 to 80 s) but immobility returned to control levels at the next dose (1 μg). At higher doses, immobility decreased monotonically, with a second MED of 16 μg and a maximal effect (36 s) at 32 μg. (+)8-OH-DPAT and F13714 also diminished immobility but, unlike NLX-101, they did so in a unimodal manner, with MEDs of 1 and 4 μg, and maximal responses of 31 and 4 s, for (+)8-OH-DPAT and F13714, respectively. The effects of (+)8-OH-DPAT (16 μg) and of both active doses of NLX-101 (0.25 and 16 μg) were prevented by the 5-HT1A receptor antagonist WAY-100,635 (0.63 mg/kg s.c.). In conclusion, activation of 5-HT1A receptors in the PFC by NLX-101 produces robust antidepressant-like effects in the rat FST, with a distinctive bimodal dose-response pattern. These data suggest that NLX-101 may target specific 5-HT1A receptor subpopulations in PFC, likely located on GABAergic and/or glutamatergic neurons. Reference: Behav Brain Res. 2021 Mar 5;401:113082. https://linkinghub.elsevier.com/retrieve/pii/S0166-4328(20)30781-6 |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 200.0 | 506.50 |
The following data is based on the product molecular weight 394.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: | 1. Depoortère R, Auclair AL, Newman-Tancredi A. NLX-101, a highly selective 5-HT1A receptor biased agonist, mediates antidepressant-like activity in rats via prefrontal cortex 5-HT1A receptors. Behav Brain Res. 2021 Mar 5;401:113082. doi: 10.1016/j.bbr.2020.113082. Epub 2020 Dec 25. PMID: 33358917. 2. Lladó-Pelfort L, Assié MB, Newman-Tancredi A, Artigas F, Celada P. 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. doi: 10.1111/j.1476-5381.2010.00738.x. PMID: 20649591; PMCID: PMC2958639. |
1: Huot P, Johnston TH, Fox SH, Newman-Tancredi A, Brotchie JM. The highly-selective 5-HT(1A) agonist F15599 reduces L-DOPA-induced dyskinesia without compromising anti-parkinsonian benefits in the MPTP-lesioned macaque. Neuropharmacology. 2015 Oct;97:306-11. doi: 10.1016/j.neuropharm.2015.05.033. Epub 2015 Jun 10. PubMed PMID: 26071982.
