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| 5mg |
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| Targets |
The compound targets the TrkA receptor, a tyrosine kinase receptor for nerve growth factor (NGF). It is a partial agonist of TrkA. Tavilermide demonstrates activities similar to NGF but does not bind to the p75NTR receptor. It can potentiate the effects of suboptimal concentrations of NGF.
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| ln Vitro |
For the treatment of dry eye, tyrosine kinase TrkA receptor agonist tavilermide (MIM-D3) is used. Tavilermide is a cyclic peptide mimetic that is proteolytically stable and has been demonstrated to be a partial agonist of the TrkA receptor. Tavilermide can amplify the effects of NGF at less-than-ideal concentrations and functions similarly to NGF (but does not bind to the p75NTR receptor) [1].
In vitro, Tavilermide is a tyrosine kinase TrkA receptor agonist. It is a proteolytically stable, cyclic peptidomimetic that has been shown to be a partial TrkA receptor agonist. It demonstrates activities similar to NGF and can potentiate the effects of suboptimal concentrations of NGF. |
| ln Vivo |
Tavilermide has been investigated for the treatment of dry eye syndrome (keratoconjunctivitis sicca). As an NGF mimetic, it is designed to mimic the biological activity of NGF, which plays a critical role in the growth and survival of nerve cells. It has been evaluated in clinical trials for dry eye.
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| Enzyme Assay |
Tavilermide is a peptide mimetic. In vitro receptor binding and functional assays would involve measuring its affinity and activity at the TrkA receptor. Cells expressing TrkA are treated with varying concentrations of Tavilermide. Receptor activation is measured by assessing TrkA phosphorylation or downstream signaling pathways. EC50 values are calculated from concentration-response curves.
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| Cell Assay |
For in vitro cell-based assays, cells expressing TrkA receptors are cultured and treated with Tavilermide at various concentrations. Receptor activation is measured by assessing TrkA phosphorylation by Western blot or by measuring downstream signaling. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo animal studies for Tavilermide would typically use models of dry eye disease. The compound is administered topically as an ophthalmic solution. Tear production, corneal damage, and inflammation are assessed. Clinical trials have been conducted in patients with dry eye.
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| ADME/Pharmacokinetics |
Tavilermide (CAS 263251-78-1) has a molecular formula of C24H32N6O11 and a molecular weight of 580.54. It is a solid. It should be stored as a powder at -20°C for 3 years or in solvent at -80°C for 6 months. Detailed pharmacokinetic parameters are not extensively characterized.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Tavilermide are not extensively provided. As a TrkA receptor partial agonist, it would be expected to have a safety profile related to NGF signaling. It has been evaluated in clinical trials for dry eye. Standard toxicology assessments would be required for therapeutic development.
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| References | |
| Additional Infomation |
Tavimid has been studied for its potential use in treating dry eye syndrome.
Tavilermide (MIM-D3) is a proteolytically stable, cyclic peptidomimetic that is a partial TrkA receptor agonist. It is an NGF mimetic. It has been investigated for the treatment of dry eye syndrome and has been evaluated in a randomized, placebo-controlled Phase 2 clinical trial. No approved therapeutic status is reported. |
| Molecular Formula |
C24H32N6O11
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|---|---|
| Molecular Weight |
580.544486045837
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| Exact Mass |
580.213
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| CAS # |
263251-78-1
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| PubChem CID |
9808372
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| Appearance |
White to off-white solid powder
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| LogP |
1.265
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
41
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| Complexity |
988
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1COC2=C(C=C(C=C2)[N+](=O)[O-])C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H]1C(=O)NCC(=O)O)CCCCN)CCC(=O)O
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| InChi Key |
DVJXNXPFYJIACK-ULQDDVLXSA-N
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| InChi Code |
InChI=1S/C24H32N6O11/c25-9-2-1-3-15-23(37)29-17(22(36)26-12-20(33)34)8-10-41-18-6-4-13(30(39)40)11-14(18)21(35)27-16(24(38)28-15)5-7-19(31)32/h4,6,11,15-17H,1-3,5,7-10,12,25H2,(H,26,36)(H,27,35)(H,28,38)(H,29,37)(H,31,32)(H,33,34)/t15-,16-,17-/m0/s1
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| Chemical Name |
3-[(5S,8S,11S)-8-(4-aminobutyl)-5-(carboxymethylcarbamoyl)-16-nitro-7,10,13-trioxo-2-oxa-6,9,12-triazabicyclo[12.4.0]octadeca-1(14),15,17-trien-11-yl]propanoic 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) |
NH4OH : 50 mg/mL (~86.13 mM)
H2O : ~2 mg/mL (~3.45 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 4.17 mg/mL (7.18 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
Solubility in Formulation 2: 25 mg/mL (43.06 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 10 mg/mL (17.23 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7225 mL | 8.6127 mL | 17.2253 mL | |
| 5 mM | 0.3445 mL | 1.7225 mL | 3.4451 mL | |
| 10 mM | 0.1723 mL | 0.8613 mL | 1.7225 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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