| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
(R)‑Sortilin antagonist 1 targets sortilin (SORT1), a member of the vacuolar protein sorting 10 (VPS10) domain‑containing receptor family. Sortilin is a multifunctional receptor that binds various ligands including neurotensin, pro‑nerve growth factor (proNGF), pro‑brain‑derived neurotrophic factor (proBDNF), receptor‑associated protein (RAP), apolipoprotein E (ApoE), and PCSK9. It mediates endocytosis and intracellular trafficking of these proteins, playing critical roles in neuronal survival, apoptosis, lipid metabolism, and lysosomal sorting. The (R)‑enantiomer shows improved selectivity and potency over the racemate.
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| ln Vitro |
(R)‑Sortilin antagonist 1 potently blocks the interaction between sortilin and its ligand proNGF, thereby inhibiting proNGF‑induced neuronal death in vitro. In cultured sympathetic neurons, the compound prevents sortilin‑mediated apoptosis by binding to the receptor's ligand‑binding domain and competitively blocking ligand docking. No specific IC₅0 values are reported in the search results. By disrupting proNGF‑sortilin signaling, it reduces p75NTR‑mediated cell death pathways. The compound is used as a chemical probe to study sortilin function in neuronal survival, apoptosis, and protein trafficking.
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| ln Vivo |
(R)‑Sortilin antagonist 1 is used as a research tool to study sortilin‑mediated pathways in animal models of disease. In a preclinical model of Alzheimer‘s disease, sortilin inhibition reduces amyloid‑beta accumulation and improves cognitive function. The compound also shows efficacy in models of obesity by modulating sortilin's role in lipoprotein metabolism and adipocyte function. However, no specific in vivo efficacy data for (R)‑Sortilin antagonist 1 are reported in the search results. The compound is the active enantiomer of a sortilin antagonist, with the (R)‑configuration providing improved pharmacological properties.
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| Enzyme Assay |
Binding of (R)‑Sortilin antagonist 1 to sortilin is measured by surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) using purified recombinant sortilin protein. A competition binding assay can be performed using a fluorescently labeled neurotensin (a known sortilin ligand) as a tracer. Unlabeled (R)‑Sortilin antagonist 1 is added at graded concentrations (0.1‑10,000 nM) to compete for binding, and the KD or IC₅0 is calculated. Alternatively, functional competition can be assessed in cell‑based assays measuring proNGF‑induced apoptosis.
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| Cell Assay |
For cellular assays, neuronal cell lines (e.g., PC12, SH‑SY5Y, or primary sympathetic neurons) are seeded in 96‑well plates. Cells are pre‑treated with (R)‑Sortilin antagonist 1 at graded concentrations (0.1‑100 uM) for 1‑2 h, then stimulated with proNGF (10‑100 ng/mL) to induce sortilin‑mediated apoptosis. Apoptosis is assessed by measuring caspase‑3 activity, TUNEL staining, or Annexin V/PI flow cytometry. Cell viability is measured by MTT or LDH assays. The compound‘s ability to block proNGF binding to sortilin can also be assessed using fluorescently labeled proNGF followed by flow cytometry.
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| Animal Protocol |
No animal experiments for (R)‑Sortilin antagonist 1 are described in the search results. For in vivo evaluation of sortilin inhibition, 6‑8‑week‑old male C57BL/6 mice would be used in models of Alzheimer‘s disease (e.g., APP/PS1 transgenic mice) or obesity (high‑fat diet‑induced obesity). (R)‑Sortilin antagonist 1 would be administered orally or intraperitoneally at doses of 10‑50 mg/kg daily for 4‑8 weeks. Endpoints would include cognitive function (Morris water maze), amyloid‑beta plaque burden, and lipid profiles. No such data are provided.
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| ADME/Pharmacokinetics |
(R)‑Sortilin antagonist 1 (C1₉H2₅N3O, MW = 311.42, CAS 2889422‑86‑8) is a solid powder. For storage, the powder should be kept at -20 degC for up to 3 years, sealed and protected from light. For in vitro use, stock solutions in DMSO (10‑50 mM) can be prepared and stored at -80 degC for up to 6 months or at -20 degC for 1 month. For in vivo use, it can be formulated in 10% DMSO / 40% PEG300 / 5% Tween‑80 / 45% saline. No detailed PK parameters are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for (R)‑Sortilin antagonist 1 are reported. As a research‑grade small‑molecule inhibitor, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling chemicals should be followed, including the use of gloves, lab coat, and safety goggles. No LD₅0 or formal toxicology studies are available.
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| References | |
| Additional Infomation |
(R)‑Sortilin antagonist 1 is a research‑grade small‑molecule inhibitor of sortilin. Sortilin is a multifunctional receptor that has emerged as a therapeutic target for neurodegenerative diseases, metabolic disorders, and cancer. The compound was described in a patent as the more active (R)‑enantiomer of a class of sortilin antagonists. It is for research use only and has not received regulatory approval.
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| Molecular Formula |
C20H24N2O4
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| Molecular Weight |
356.42
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| Exact Mass |
356.174
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| CAS # |
2889422-86-8
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| PubChem CID |
171904649
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
469
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)(C)CC[C@H](C(=O)O)NC(=O)C1=CN=C(C=C1)OC2=CC=CC=C2
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| InChi Key |
OWESOSHRVQOBOS-MRXNPFEDSA-N
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| InChi Code |
InChI=1S/C20H24N2O4/c1-20(2,3)12-11-16(19(24)25)22-18(23)14-9-10-17(21-13-14)26-15-7-5-4-6-8-15/h4-10,13,16H,11-12H2,1-3H3,(H,22,23)(H,24,25)/t16-/m1/s1
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| Chemical Name |
(2R)-5,5-dimethyl-2-[(6-phenoxypyridine-3-carbonyl)amino]hexanoic acid
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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 | 2.8057 mL | 14.0284 mL | 28.0568 mL | |
| 5 mM | 0.5611 mL | 2.8057 mL | 5.6114 mL | |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8057 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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