| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TrkB
Cyclotraxin B targets TrkB, the primary receptor for Brain-Derived Neurotrophic Factor (BDNF). It functions as a negative allosteric modulator, meaning it binds to a site distinct from the BDNF binding site and inhibits receptor activation non-competitively. It does not interfere with BDNF binding but prevents BDNF-induced TrkB activation. |
|---|---|
| ln Vitro |
In vitro, Cyclotraxin B inhibits BDNF-induced TrkB activity in a kinase receptor activation ELISA (KIRA-ELISA) using tetracycline-responsive CHO-K1 cells expressing recombinant human TrkB (TetOn-rhTrkB cells) with an IC50 of 0.3 nM. Its inhibitory activity is typically assessed using cell-based assays that measure TrkB phosphorylation in response to BDNF.
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| ln Vivo |
In vivo, Cyclotraxin B has been shown to have analgesic and anxiolytic effects. Its ability to cross the blood-brain barrier allows it to modulate TrkB signaling in the central nervous system. These studies provide evidence for its potential therapeutic applications in pain and anxiety disorders.
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| Enzyme Assay |
Cell-free assays for Cyclotraxin B typically involve measuring its binding affinity to TrkB using surface plasmon resonance (SPR) or radioligand binding assays. These assays are used to characterize the compound's potency and mechanism of action as a negative allosteric modulator.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of Cyclotraxin B. Cells expressing TrkB are treated with BDNF in the presence or absence of the compound, and TrkB phosphorylation is measured to assess the inhibition of BDNF-induced signaling. These assays confirm that Cyclotraxin B effectively blocks TrkB-mediated cellular responses without interfering with BDNF binding.
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| Animal Protocol |
In vivo animal experiments typically involve rodent models of pain or anxiety. Animals are administered Cyclotraxin B via injection. Behavioral tests are used to assess its analgesic and anxiolytic effects. TrkB phosphorylation in brain tissues is measured to confirm target engagement. These studies provide evidence for the compound's therapeutic potential.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Cyclotraxin B are characteristic of a cyclic peptide. Its molecular weight is 1200.36. Its ability to cross the blood-brain barrier suggests it has favorable properties for central nervous system targeting. Its pharmacokinetic profile, including half-life and bioavailability, is not fully characterized but supports its use in research.
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| Toxicity/Toxicokinetics |
The toxicity profile of Cyclotraxin B is not extensively documented. As a peptide, it is generally considered to have low toxicity. In preclinical studies, the compound has been shown to be well-tolerated at therapeutic doses, with a safety profile that supports its use in research.
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| References |
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| Additional Infomation |
Cyclotraxin B is a research compound used to study TrkB signaling and its role in pain, anxiety, and other neurological disorders. It is a selective, potent negative allosteric modulator of TrkB. The compound is not approved for therapeutic use and is intended for research purposes only.
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| Molecular Formula |
C48H73N13O17S3
|
|---|---|
| Molecular Weight |
1200.36512732506
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| Exact Mass |
1199.44
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| CAS # |
1203586-72-4
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| Related CAS # |
Cyclotraxin B TFA
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| PubChem CID |
90489002
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| Appearance |
White to off-white solid powder
|
| LogP |
-9
|
| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
81
|
| Complexity |
2230
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| Defined Atom Stereocenter Count |
10
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| SMILES |
S(C)CC[C@H]1C(NCC(N[C@H](C(N[C@@H]([C@@H](C)O)C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(=O)O)CSSC[C@@H](C(N[C@@H](CC(N)=O)C(N2CCC[C@H]2C(N1)=O)=O)=O)N)=O)=O)CCC(=O)O)=O)CCCCN)=O)=O)CC1C=CC(=CC=1)O)=O)=O
|
| InChi Key |
JLBMMJHZUYBFGX-ZHTCEXBHSA-N
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| InChi Code |
InChI=1S/C48H73N13O17S3/c1-24(62)39-46(75)58-28(6-3-4-15-49)43(72)56-29(12-13-38(67)68)41(70)52-21-37(66)55-33(48(77)78)23-81-80-22-27(50)40(69)59-32(19-35(51)64)47(76)61-16-5-7-34(61)45(74)57-30(14-17-79-2)42(71)53-20-36(65)54-31(44(73)60-39)18-25-8-10-26(63)11-9-25/h8-11,24,27-34,39,62-63H,3-7,12-23,49-50H2,1-2H3,(H2,51,64)(H,52,70)(H,53,71)(H,54,65)(H,55,66)(H,56,72)(H,57,74)(H,58,75)(H,59,69)(H,60,73)(H,67,68)(H,77,78)/t24-,27+,28+,29+,30+,31+,32+,33+,34+,39+/m1/s1
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| Chemical Name |
(3S,6R,11R,17S,20S,23S,26S,32S,35S)-6-amino-20-(4-aminobutyl)-3-(2-amino-2-oxoethyl)-17-(2-carboxyethyl)-23-[(1R)-1-hydroxyethyl]-26-[(4-hydroxyphenyl)methyl]-32-(2-methylsulfanylethyl)-2,5,13,16,19,22,25,28,31,34-decaoxo-8,9-dithia-1,4,12,15,18,21,24,27,30,33-decazabicyclo[33.3.0]octatriacontane-11-carboxylic 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O: 100 mg/mL (83.31 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (83.31 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8331 mL | 4.1654 mL | 8.3308 mL | |
| 5 mM | 0.1666 mL | 0.8331 mL | 1.6662 mL | |
| 10 mM | 0.0833 mL | 0.4165 mL | 0.8331 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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