| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
NTRC-824 targets the neurotensin receptor type 2 (NTS2), a G-protein-coupled receptor that binds the neuropeptide neurotensin. NTS2 is involved in the regulation of pain, mood, and neuroendocrine functions. As a selective NTS2 antagonist, NTRC-824 blocks neurotensin-mediated signaling at NTS2 with high potency (IC₅₀ = 38 nM) and exceptional selectivity over NTS1.
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| ln Vitro |
Upon testing NTRC-824 (Compound 5) at the NTS1 receptor, no binding activity was seen in NTS1 assays up to 30 μM. Therefore, in binding and functional assays, NTRC-824 (Compound 5) was selective for NTS2. The first non-peptide molecule that functions like an endogenous ligand and is more potent than one is NTRC-824 (compound 5) [1].
In vitro, NTRC-824 acts as a potent and selective NTS2 antagonist with an IC₅₀ of 38 nM and a Kᵢ of 202 nM. It exhibits >150-fold selectivity for NTS2 over NTS1, with a Kᵢ >30 µM for NTS1. Its in vitro activity is assessed using receptor binding and functional assays measuring neurotensin-induced signaling. |
| ln Vivo |
NTRC-824 is an orally active, CNS-penetrant compound used in preclinical research. Its in vivo activity is studied in animal models to investigate the role of NTS2 in pain, mood disorders, and neuroendocrine function. The compound serves as a valuable tool for studying NTS2-mediated pathways.
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| Enzyme Assay |
The in vitro receptor binding assay for NTRC-824 involves measuring its affinity for the NTS2 receptor using radioligand binding techniques. These assays use membrane preparations from cells expressing the NTS2 receptor and measure the displacement of a labeled ligand by the compound. IC₅₀ of 38 nM and Kᵢ of 202 nM are determined for NTS2. Selectivity over NTS1 (Kᵢ >30 µM) is also assessed.
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| Cell Assay |
In vitro cellular assays for NTRC-824 are performed using cells expressing the human NTS2 receptor. These assays measure the compound's ability to antagonize neurotensin-induced signaling, such as calcium mobilization or other downstream pathways. The compound's potent and selective NTS2 antagonism is demonstrated by its ability to inhibit NTS2-mediated effects without affecting NTS1.
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| Animal Protocol |
In vivo animal studies for NTRC-824 are conducted in rodent models to assess its effects on NTS2-mediated functions. These studies typically involve administration of the compound, followed by assessment of pain responses, mood-related behaviors, or neuroendocrine parameters. The compound's CNS penetration and oral activity support its use in these studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NTRC-824 are characterized by oral activity and central nervous system penetration. The compound has a molecular formula of C₂₅H₂₆F₃N₃O₆S and a molecular weight of 553.55 g/mol. It is soluble in DMSO (55.35 mg/mL) and should be stored at -20°C. Its pharmacokinetic profile supports CNS research applications.
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| Toxicity/Toxicokinetics |
Toxicology studies of NTRC-824 have been conducted to support its use in preclinical research. As a CNS-penetrant compound, its toxicology profile includes effects on the central nervous system and potential for off-target effects at other neurotensin receptors or related GPCRs. The compound is for research use only.
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| References | |
| Additional Infomation |
NTRC-824 (CAS: 1623002-61-8) is a potent, selective non-peptide antagonist of the neurotensin receptor type 2 (NTS2) with an IC₅₀ of 38 nM and a Kᵢ of 202 nM. It exhibits >150-fold selectivity for NTS2 over NTS1. The compound has a molecular formula of C₂₅H₂₆F₃N₃O₆S and a molecular weight of 553.55 g/mol. It is for research use only.
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| Molecular Formula |
C25H26F3N3O6S
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|---|---|
| Molecular Weight |
553.550655841827
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| Exact Mass |
553.149
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| CAS # |
1623002-61-8
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| PubChem CID |
101873359
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
38
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| Complexity |
976
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S(C1C=CC(C)=CC=1)(NC1C=CC2=C(C=1)C(C(C(F)(F)F)=O)=CN2CC(N[C@H](C(=O)O)CC(C)C)=O)(=O)=O
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| InChi Key |
SOOLLEBJNGCDOZ-FQEVSTJZSA-N
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| InChi Code |
InChI=1S/C25H26F3N3O6S/c1-14(2)10-20(24(34)35)29-22(32)13-31-12-19(23(33)25(26,27)28)18-11-16(6-9-21(18)31)30-38(36,37)17-7-4-15(3)5-8-17/h4-9,11-12,14,20,30H,10,13H2,1-3H3,(H,29,32)(H,34,35)/t20-/m0/s1
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| Chemical Name |
(2S)-4-methyl-2-[[2-[5-[(4-methylphenyl)sulfonylamino]-3-(2,2,2-trifluoroacetyl)indol-1-yl]acetyl]amino]pentanoic acid
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| Synonyms |
NTRC824; NTRC 824; NTRC-824
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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 | 1.8065 mL | 9.0326 mL | 18.0652 mL | |
| 5 mM | 0.3613 mL | 1.8065 mL | 3.6130 mL | |
| 10 mM | 0.1807 mL | 0.9033 mL | 1.8065 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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