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Purity: ≥98%
| Targets |
STAT3; Colivelin is an activator of signal transducer and activator of transcription 3 (STAT3); Amyloid-β
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| ln Vitro |
At a concentration of 100 fm, colavelin totally inhibits mortality caused by overexpressed FAD-caused genes and Aβ1-43, while maintaining its neuroprotective effects at or above 1 nm[1]. Colivelin-induced neuroprotection is mediated by two neuroprotective pathways: signal transducer and activator of transcription 3 (STT3), which is initiated by HN, and Ca2+/calmodulin-dependent protein kinase IV, which is mediated by ADNF[1]. In HT22 cells treated with rmMFG -E8, collagen reverses the expressions of caspase-3, Bax, and Bcl-2 in the co-cultured cells under OGD conditions[4]. In BV-2 cells, ivelin (50 µg/mL, 4 hours) dramatically raises the levels of the protein p-STAT3[4].
Colivelin can significantly increase the phosphorylation level of STAT3 in vitro. It can completely inhibit the cell death induced by specific pathogenic genes and Aβ1 - 43 at a concentration of 100 fM, and has a long - term beneficial effect on neurodegenerative disease symptoms such as neurotoxicity, Aβ deposition, neuronal apoptosis and synaptic plasticity defects. The mechanism may be related to the activation of the JAK/STAT3 signaling pathway, up - regulating the expression of anti - apoptotic genes, thus protecting neurons from damage [1] |
| ln Vivo |
Colivelin (intracerebroventricular administration; 10 pmol/3 μl; 3 weeks) antagonizes neuronal loss in the CA1 region of the hippocampus by injecting Aβ1-42 into the hippocampal region, and it suppresses impairment in spatial working-induced memory induced by repetitive intracerebroventricular injection of Aβ25-35 or Aβ1-42[1]. Colivelin suppresses memory impairment caused by 3-quinuclidinyl benzilate and restricts functional memory deficit when administered intraperitoneally at 1.4, 7, or 35 nM/0.21 mL on the Y-maze test day[1]. (intraperitoneal injection; 1 mg/kg; 14 days) over time, as measured by the mNSS, rotarod, and corner turning tests, improves motor and cognitive function. Additionally, it improves neurological deficits following MCAO and decreases lesion volume[1].
Colivelin can effectively prevent memory impairment in vivo. Whether administered intraperitoneally or intracerebroventricularly, it can improve spatial working memory impairment, neuronal loss and memory impairment in animal models. In the mouse middle cerebral artery occlusion (MCAO) model, it can alleviate ischemic brain injury and improve the neurological function score. The mechanism is to activate the JAK/STAT3 signaling pathway, up - regulate the expression of anti - apoptotic genes such as Bcl - 2, and inhibit the expression of pro - apoptotic genes such as Bax, thereby reducing neuronal death during ischemia - reperfusion injury [1] |
| 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: 0.5 μM. Incubation Duration: 1 hour (followed by CYT-Rx20 treatment) Experimental Results: Dramatically suppressed the viability in KYSE70 and TE8 cells. Take BV - 2 cells as the research object, construct an oxygen - glucose deprivation (OGD) model, and then treat the cells with Colivelin. Use Western blot to detect the protein level of p - STAT3, and detect the expression of related proteins such as suppressor of cytokine signaling 3 (SOCS3) to analyze the role of Colivelin in intracellular signal regulation [3] |
| Animal Protocol |
Animal/Disease Models: CD-1 mice[1]
Doses: 10 pmol/3 μl Route of Administration: Intracerebroventricular administration Experimental Results: Completely suppressed Aβ 25-35-mediated impairment in spatial working memory and increased the number of immunoreactive neurons. Animal/Disease Models: C57 mice[1] Doses: 1.4, 7, or 35 nM/0.21mL Route of Administration: intraperitoneal (ip)administration Experimental Results: Protected against cholinotoxin-induced amnesia in mice. Animal/Disease Models: Male C57BL/ 6 mice[3] Doses: 1 mg/kg Route of Administration: intraperitoneal (ip)administration Experimental Results: Protected against ischemic brain injury, and improves neurological outcomes. Dissolve Colivelin in an appropriate solvent (the literature does not specify the specific solvent, it can be inferred according to the solubility that it can be dissolved in water). In the study of memory impairment, it can be administered intraperitoneally or intracerebroventricularly; in the mouse MCAO model, the specific administration frequency is not mentioned in the literature, and it can be administered once a day, and the dosage is not specified either. Observe the change of neurological function score after administration, and take brain tissue for relevant index detection [1] |
| References |
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| Additional Infomation |
Colivelin is a femtomolar - acting humanin derivative, which is composed of activity - dependent neurotrophic factor (ADNF) C - terminally fused to AGA - (C8R) HNG17. It has good brain permeability and can cross the blood - brain barrier. It has a neuroprotective effect on Alzheimer's disease and ischemic brain injury, and can be used as a potential drug for the treatment of neurodegenerative diseases [1]
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| Molecular Formula |
C121H207F3N32O37
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|---|---|
| Molecular Weight |
2759.13
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| Exact Mass |
2760.544
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| CAS # |
2803948-60-7
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| Related CAS # |
867021-83-8
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| PubChem CID |
170907493
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| Sequence |
H-Ser-Ala-Leu-Leu-Arg-Ser-Ile-Pro-Ala-Pro-Ala-Gly-Ala-Ser-Arg-Leu-Leu-Leu-Leu-Thr-Gly-Glu-Ile-Asp-Leu-Pro-OH.TFA; Ser-Ala-Leu-Leu-Arg-Ser-Ile-Pro-Ala-Pro-Ala-Gly-Ala-Ser-Arg-Leu-Leu-Leu-Leu-Thr-Gly-Glu-Ile-Asp-Leu-Pro;
L-seryl-L-alanyl-L-leucyl-L-leucyl-L-arginyl-L-seryl-L-isoleucyl-L-prolyl-L-alanyl-L-prolyl-L-alanyl-glycyl-L-alanyl-L-seryl-L-arginyl-L-leucyl-L-leucyl-L-leucyl-L-leucyl-L-threonyl-glycyl-L-alpha-glutamyl-L-isoleucyl-L-alpha-aspartyl-L-leucyl-L-proline trifluoroacetic acid
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| SequenceShortening |
SALLRSIPAPAGASRLLLLTGEIDLP
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
38
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| Hydrogen Bond Acceptor Count |
44
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| Rotatable Bond Count |
86
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| Heavy Atom Count |
193
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| Complexity |
5990
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| Defined Atom Stereocenter Count |
27
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| SMILES |
C(N1CCC[C@H]1C(=O)N[C@@H](C)C(N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@]([H])([C@H](O)C)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@]([H])([C@@H](C)CC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(N1CCC[C@H]1C(=O)O)=O)=O)(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO.C(F)(F)(F)C(=O)O
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| InChi Key |
LVLDZLQHAOAKIR-MZNINCGGSA-N
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| InChi Code |
InChI=1S/C119H208N32O35.C2HF3O2/c1-24-63(17)91(113(181)142-80(50-90(160)161)106(174)143-81(49-62(15)16)115(183)151-42-30-35-86(151)117(185)186)146-100(168)73(36-37-89(158)159)133-88(157)52-128-112(180)93(69(23)155)148-107(175)79(48-61(13)14)141-105(173)78(47-60(11)12)140-104(172)77(46-59(9)10)139-103(171)76(45-58(7)8)137-98(166)71(31-26-38-125-118(121)122)135-108(176)82(54-153)144-95(163)66(20)129-87(156)51-127-94(162)65(19)131-110(178)84-33-28-40-149(84)114(182)68(22)132-111(179)85-34-29-41-150(85)116(184)92(64(18)25-2)147-109(177)83(55-154)145-99(167)72(32-27-39-126-119(123)124)134-101(169)75(44-57(5)6)138-102(170)74(43-56(3)4)136-96(164)67(21)130-97(165)70(120)53-152;3-2(4,5)1(6)7/h56-86,91-93,111,132,152-155,179H,24-55,120H2,1-23H3,(H,127,162)(H,128,180)(H,129,156)(H,130,165)(H,131,178)(H,133,157)(H,134,169)(H,135,176)(H,136,164)(H,137,166)(H,138,170)(H,139,171)(H,140,172)(H,141,173)(H,142,181)(H,143,174)(H,144,163)(H,145,167)(H,146,168)(H,147,177)(H,148,175)(H,158,159)(H,160,161)(H,185,186)(H4,121,122,125)(H4,123,124,126);(H,6,7)/t63-,64-,65-,66-,67-,68-,69+,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,91-,92-,93-,111?;/m0./s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]pyrrolidin-2-yl]-hydroxymethyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]acetyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carboxylic acid;2,2,2-trifluoroacetic acid
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| Synonyms |
Colivelin TFA; orb1679763; 2803948-60-7; (2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]pyrrolidin-2-yl]-hydroxymethyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]acetyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carboxylic acid;2,2,2-trifluoroacetic 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, 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 : 50 mg/mL (18.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 6.25 mg/mL (2.27 mM) in Water with 5% sefsol and 20% isopropanol (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3624 mL | 1.8122 mL | 3.6243 mL | |
| 5 mM | 0.0725 mL | 0.3624 mL | 0.7249 mL | |
| 10 mM | 0.0362 mL | 0.1812 mL | 0.3624 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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