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Purity: ≥98%
| ln Vitro |
Colivelin retains its neuroprotective effect at a concentration of 1 nm or above and totally prevents death induced by overexpressed FAD causal genes and Aβ1-43 [1]. Two neuroprotective routes are involved in collagen-induced neuroprotection: the first is mediated by Ca2+/calmodulin-dependent protein kinase IV and is initiated by ADNF. The second pathway is mediated by signal transducer and activator of transcription 3, which is triggered by HN[1]. Colivelin, via rmMFG-E8, can reverse the expression of caspase3, Bax, and Bcl-2 in HT22 cells that are co-cultured under OGD conditions [4]. In BV-2 cells, ivelin (50 µg/mL, 4 hours) dramatically raises the levels of the protein p-STAT3 [4].
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| ln Vivo |
The deterioration of spatial working memory brought on by recurrent intracerebroventricular injection of Aβ25-35 or Aβ1-42 can be inhibited by ivelin (intracerebroventricular treatment; 10 pmol/3 μl; 3 weeks). Furthermore, the loss of intracerebroventricular injection-induced hippocampal CA1 region neurons can be exacerbated by it. The Aβ1-42 injection[1]. Colivelin prevents 3-quinuclidinyl benzilate-induced memory impairment and limits functional memory deficits when delivered intraperitoneally at 1.4, 7, or 35 nM/0.21 mL on the day of the Y-maze test [1]. Colivelin (ip; 1 mg/kg; 14 days) gradually enhances motor and cognitive performance using mNSS, rotation, and angle tests. After MCAO, it can also lessen lesion volume and enhance neurological impairments [3].
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| Cell Assay |
Western Blot Analysis[4]
Cell Types: BV-2 cells. Tested Concentrations: 50 µg/mL. Incubation Duration: 4 hrs (hours). Experimental Results: Increased p-STAT3 levels. Cell viability assay[5] Cell Types: KYSE70 and TE8 cells. Tested Concentrations: 0.5μM. Incubation Duration: 1 hour (followed by CYT-Rx20 treatment) Experimental Results: Dramatically inhibited the viability of KYSE70 and TE8 cells. |
| Animal Protocol |
Animal/Disease Models: CD-1 mice [1]
Doses: 10 pmol/3 μl Route of Administration: intracerebroventricular administration Experimental Results: Completely inhibited Aβ 25-35-mediated spatial working memory impairment and increased immune-reactive neurons quantity. Animal/Disease Models: C57 mice [1] Doses: 1.4, 7 or 35 nM/0.21mL Route of Administration: intraperitonealadministration Experimental Results: Can prevent choline toxin-induced amnesia in mice. Animal/Disease Models: Male C57BL/6 mice [3] Doses: 1 mg/kg Route of Administration: intraperitonealadministration Experimental Results: Prevention of ischemic brain injury and improvement of neurological outcomes |
| References |
[1]. Chiba T, et al. Development of a femtomolar-acting humanin derivative named colivelin by attaching activity-dependent neurotrophic factor to its N terminus: characterization of colivelin-mediated neuroprotection against Alzheimer's disease-relevant insults in vitro and in vivo. J Neurosci. 2005 Nov 2;25(44):10252-61.
[2]. Pan Z, et al. Upregulation of HSP72 attenuates tendon adhesion by regulating fibroblast proliferation and collagen production via blockade of the STAT3 signaling pathway.Cell Signal. 2020 Mar 18:109606. [3]. Zhao H, et al. Colivelin Rescues Ischemic Neuron and Axons Involving JAK/STAT3 Signaling Pathway.Neuroscience. 2019 Sep 15;416:198-206. [4]. Fang YY, et al. MFG-E8 alleviates oxygen-glucose deprivation-induced neuronal cell apoptosis by STAT3 regulating the selective polarization of microglia. Int J Neurosci. 2020 Mar 12:1-10. [5]. Chiu WC, et al. The Synthetic β-Nitrostyrene Derivative CYT-Rx20 Inhibits Esophageal Tumor Growth and Metastasis via PI3K/AKT and STAT3 Pathways. PLoS One. 2016 Nov 22;11(11):e0166453. |
| Molecular Formula |
C119H206N32O35
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|---|---|
| Molecular Weight |
2645.1024
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| CAS # |
867021-83-8
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| Related CAS # |
Colivelin TFA;2803948-60-7
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C([C@]([H])([C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])N([H])/C(=N/[H])/N([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])O[H])N([H])[H])=O)=O)=O)=O)=O)=O)N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N([H])[C@@]([H])(C([H])([H])[H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N([H])[C@]([H])(C(N([H])C([H])([H])C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])O[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])C([H])([H])C(N([H])[C@@]([H])(C([H])([H])C([H])([H])C(=O)O[H])C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C(=O)O[H])C(N([H])[C@@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(=O)O[H])=O)=O)=O)[C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)=O)=O)[C@@]([H])(C([H])([H])[H])O[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)C([H])([H])C([H])([H])C([H])([H])N([H])/C(=N/[H])/N([H])[H])=O)=O)C([H])([H])[H])=O)=O)C([H])([H])[H])=O)=O)=O
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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, 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) |
DMSO : ~100 mg/mL (~37.81 mM)
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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 | 0.3781 mL | 1.8903 mL | 3.7806 mL | |
| 5 mM | 0.0756 mL | 0.3781 mL | 0.7561 mL | |
| 10 mM | 0.0378 mL | 0.1890 mL | 0.3781 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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