| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Navamepent acts as an agonist of the chemerin receptor (CMKLR1). As a resolvin E1 analog, it exerts its effects through the resolution of inflammation pathways, which are mediated by specialized pro-resolving lipid mediators. By activating CMKLR1 and potentially other resolvin E1 receptors, Navamepent promotes the active resolution of inflammation, counteracting pro-inflammatory signals and restoring tissue homeostasis. This receptor targeting underlies its therapeutic potential in inflammatory conditions of the ocular surface and other tissues.
|
|---|---|
| ln Vitro |
In vitro, Navamepent exhibits potent anti-inflammatory activity. It inhibits the release of several key pro-inflammatory mediators from corneal epithelial cells. The compound demonstrates cell survival benefits and reduces corneal epithelial damage. Its activity is consistent with its role as a resolvin E1 analog, promoting the resolution of inflammation rather than simply blocking its initiation. Navamepent also contains an alkyne group, making it a click chemistry reagent for bioconjugation applications.
|
| ln Vivo |
In vivo, Navamepent is highly effective against dry eye disease and goblet cell loss, thereby accelerating tear production. It reduces corneal inflammation and epithelial damage, and accelerates corneal tissue repair. The compound has been evaluated in clinical trials for dry eye syndrome and is also being investigated for the treatment of age-related macular degeneration and diabetic macular edema. These in vivo effects are attributed to its pro-resolving and tissue-protective activities.
|
| Enzyme Assay |
In vitro receptor binding assays for Navamepent typically involve measuring its agonistic activity at the chemerin receptor (CMKLR1). A typical protocol: HEK293 cells stably expressing human CMKLR1 are seeded in 96-well plates. Cells are treated with varying concentrations of Navamepent (0.01 nM to 10 μM) for 30-60 minutes. Receptor activation is assessed by measuring intracellular calcium mobilization using a calcium-sensitive fluorescent dye (e.g., Fluo-4 AM) or by measuring β-arrestin recruitment using a commercially available assay kit. EC₅₀ values are calculated from dose-response curves. Positive controls include chemerin or other known CMKLR1 agonists. Each concentration is tested in triplicate, and experiments are repeated at least three times.
|
| Cell Assay |
In vitro cell-based assays for Navamepent are performed using corneal epithelial cells or immune cells. A typical protocol: human corneal epithelial cells (HCEC) are seeded in 96-well plates and cultured to confluence. Cells are pre-treated with Navamepent at concentrations ranging from 0.01 to 10 μM for 1-2 hours, then stimulated with a pro-inflammatory stimulus such as TNF-α or IL-1β for 6-24 hours. Inflammatory mediator release (e.g., IL-6, IL-8, MCP-1) is measured in the culture supernatant by ELISA. Cell viability is assessed using MTT or CellTiter-Glo assays. The compound's ability to promote wound healing is assessed by scratch assay, where a monolayer is wounded and wound closure is measured after 24-48 hours of treatment. Each condition is tested in triplicate, and experiments are repeated at least three times.
|
| Animal Protocol |
In vivo animal studies for Navamepent are conducted in rodent models of dry eye disease. A typical protocol: male or female mice are treated with scopolamine and exposed to a controlled environment to induce dry eye. Navamepent is administered via topical eye drops at concentrations of 0.01-0.1% (w/v), 2-4 times daily for 7-14 days. Tear production is measured by the phenol red thread test or Schirmer's test. Corneal fluorescein staining is used to assess epithelial damage. Goblet cell density is assessed by periodic acid-Schiff (PAS) staining of conjunctival sections. Inflammatory cytokine levels in corneal tissue are measured by ELISA or qRT-PCR. Efficacy is assessed by comparing tear production, corneal staining scores, and goblet cell density between treatment and vehicle control groups.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Navamepent have been characterized in preclinical studies. The compound is administered topically (eye drops) for ophthalmic applications. It is an isopropyl ester prodrug of resolvin E1, which is likely hydrolyzed to the active resolvin E1 metabolite. The compound is soluble in DMSO (up to 100 mg/mL) and can be formulated for topical administration. Following topical ocular administration, Navamepent is expected to penetrate the corneal epithelium and reach therapeutic concentrations in ocular tissues. Its half-life in tear fluid and corneal penetration have been evaluated in preclinical models. The compound should be stored at -20°C for long-term stability (up to 3 years).
|
| Toxicity/Toxicokinetics |
Toxicological data for Navamepent have been evaluated in preclinical safety studies. In ocular toxicity studies, the compound is generally well-tolerated at therapeutic concentrations and has not been associated with significant corneal or conjunctival toxicity. The compound has not been associated with systemic toxicity at the doses used for topical administration. Standard laboratory safety precautions should be followed when handling Navamepent: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The compound should be stored at -20°C for long-term stability and protected from light and moisture. Researchers should consult the safety data sheet (SDS) before handling.
|
| References |
|
| Additional Infomation |
Additional information for Navamepent: The compound has a CAS number of 1251537-11-7. Its molecular formula is C₁₈H₂₄O₄ and molecular weight is 304.38 g/mol. The IUPAC name is propan-2-yl (5S,8E,10E,12R)-5,12-dihydroxypentadeca-8,10-dien-6,14-diynoate. Synonyms include RX-10045. The compound is a resolvin E1 analog and chemerin receptor (CMKLR1) agonist. It is an isopropyl ester prodrug of resolvin E1. It has been investigated in Phase II clinical trials for dry eye syndrome and is being studied for age-related macular degeneration and diabetic macular edema. It contains an alkyne group for click chemistry. Purity is typically ≥98%. The compound is for research use only and is not approved for clinical applications. No FDA approvals exist.
|
| Molecular Formula |
C18H24O4
|
|---|---|
| Molecular Weight |
304.386
|
| Exact Mass |
174.125
|
| Elemental Analysis |
C, 71.03; H, 7.95; O, 21.02
|
| CAS # |
1251537-11-7
|
| PubChem CID |
46926878
|
| Appearance |
Yellow to brown liquid（Density：1.088±0.06 g/cm3）
|
| Density |
1.0±0.1 g/cm3
|
| Boiling Point |
227.4±23.0 °C at 760 mmHg
|
| Flash Point |
82.9±15.4 °C
|
| Vapour Pressure |
0.0±1.0 mmHg at 25°C
|
| Index of Refraction |
1.438
|
| LogP |
1.29
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
22
|
| Complexity |
493
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O(C(C)C)C(CCC[C@@H](C#C/C=C/C=C/[C@@H](CC#C)O)O)=O
|
| InChi Key |
ZVOCIIHCJJEFRQ-BHXBHYJPSA-N
|
| InChi Code |
InChI=1S/C18H24O4/c1-4-10-16(19)11-7-5-6-8-12-17(20)13-9-14-18(21)22-15(2)3/h1,5-7,11,15-17,19-20H,9-10,13-14H2,2-3H3/b6-5+,11-7+/t16-,17-/m1/s1
|
| Chemical Name |
propan-2-yl (5S,8E,10E,12R)-5,12-dihydroxypentadeca-8,10-dien-6,14-diynoate
|
| Synonyms |
RX10045; RX-10045; Navamepent; 1251537-11-7; RX-10,045; Q7789B8MWM; propan-2-yl (5S,8E,10E,12R)-5,12-dihydroxypentadeca-8,10-dien-6,14-diynoate; .
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~328.54 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2853 mL | 16.4263 mL | 32.8526 mL | |
| 5 mM | 0.6571 mL | 3.2853 mL | 6.5705 mL | |
| 10 mM | 0.3285 mL | 1.6426 mL | 3.2853 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
