| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
ApoA-I mimetic peptide exhibits potent activation of lecithin:cholesterol acyltransferase (LCAT), an enzyme responsible for the esterification of cholesterol in HDL particles. By activating LCAT, the peptide promotes reverse cholesterol transport and HDL maturation.
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|---|---|
| ln Vitro |
The peptide demonstrates good LCAT activation potency in vitro. It can be used for the synthesis of peptide/lipid complexes, which are valuable tools in cardiovascular and metabolic research. Cellular assays typically utilize macrophage cell lines to measure cholesterol efflux.
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| ln Vivo |
In vivo, ApoA-I mimetic peptides are employed in animal models to evaluate their effects on foam cell formation, macrophage lipid handling, and atherosclerotic lesion development. These peptides have been shown to reduce atherosclerosis progression in various mouse models.
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| Enzyme Assay |
In vitro LCAT activation assays are performed by incubating the peptide with synthetic lipid substrates (phosphatidylcholine/cholesterol liposomes) and purified LCAT enzyme. The reaction is monitored by measuring the formation of cholesteryl esters using radiometric or chromatographic methods. Activity is expressed as the percentage of cholesterol esterified per unit time.
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| Cell Assay |
Cellular assays for ApoA-I mimetic peptide typically utilize macrophage cell lines (e.g., RAW 264.7 or THP-1-derived macrophages) to measure cholesterol efflux. Cells are loaded with fluorescently or radiolabeled cholesterol, then incubated with the peptide. The amount of cholesterol released into the medium is measured and compared to control treatments.
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| Animal Protocol |
In vivo animal studies typically use atherosclerosis-prone mouse models such as ApoE-deficient or LDL receptor-deficient mice. Peptides are administered via intraperitoneal or subcutaneous injection, and atherosclerosis progression is assessed by quantifying aortic lesion area. Lipid profiles, inflammatory markers, and macrophage cholesterol content are also evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ApoA-I mimetic peptides are characteristic of peptide therapeutics, typically exhibiting rapid clearance from circulation with half-lives ranging from minutes to a few hours. The peptide is subject to proteolytic degradation and renal clearance.
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| Toxicity/Toxicokinetics |
As a peptide-based research compound, ApoA-I mimetic peptide is generally well-tolerated in animal studies at research doses. Standard safety precautions for handling synthetic peptides should be followed. No significant toxicity has been reported in the literature for this specific peptide.
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| References |
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| Additional Infomation |
ApoA-I mimetic peptide is a valuable tool in cardiovascular research for studying HDL function, reverse cholesterol transport, and atherosclerosis pathogenesis. It has been investigated in preclinical models as a potential therapeutic agent for cardiovascular disease. The peptide is also used in the synthesis of peptide/lipid complexes. At least 30 references in Google Scholar cite research involving this peptide.
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| Molecular Formula |
C122H208N30O33
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|---|---|
| Molecular Weight |
2623.13815021515
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| Exact Mass |
2622.555
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| CAS # |
221882-20-8
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| PubChem CID |
171706663
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| Sequence |
Pro-Val-Leu-Asp-Leu-Phe-Arg-Glu-Leu-Leu-Asn-Glu-Leu-Leu-Glu-Ala-Leu-Lys-Gln-Lys-Leu-Lys
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| SequenceShortening |
PVLDLFRELLNELLEALKQKLK
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
35
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| Hydrogen Bond Acceptor Count |
38
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| Rotatable Bond Count |
95
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| Heavy Atom Count |
185
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| Complexity |
5710
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| Defined Atom Stereocenter Count |
22
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| SMILES |
C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2
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| InChi Key |
OTFKMDYRWGESRW-BIACLGMUSA-N
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| InChi Code |
InChI=1S/C122H208N30O33/c1-62(2)51-82(109(172)134-74(33-23-26-46-123)103(166)136-77(38-42-93(126)153)106(169)133-75(34-24-27-47-124)105(168)142-84(53-64(5)6)111(174)140-81(121(184)185)35-25-28-48-125)141-100(163)71(19)132-102(165)78(39-43-95(155)156)138-110(173)83(52-63(3)4)145-112(175)85(54-65(7)8)144-108(171)80(41-45-97(159)160)139-118(181)91(60-94(127)154)149-115(178)88(57-68(13)14)146-113(176)86(55-66(9)10)143-107(170)79(40-44-96(157)158)137-104(167)76(37-30-50-131-122(128)129)135-117(180)90(59-72-31-21-20-22-32-72)148-114(177)87(56-67(11)12)147-119(182)92(61-98(161)162)150-116(179)89(58-69(15)16)151-120(183)99(70(17)18)152-101(164)73-36-29-49-130-73/h20-22,31-32,62-71,73-92,99,130H,23-30,33-61,123-125H2,1-19H3,(H2,126,153)(H2,127,154)(H,132,165)(H,133,169)(H,134,172)(H,135,180)(H,136,166)(H,137,167)(H,138,173)(H,139,181)(H,140,174)(H,141,163)(H,142,168)(H,143,170)(H,144,171)(H,145,175)(H,146,176)(H,147,182)(H,148,177)(H,149,178)(H,150,179)(H,151,183)(H,152,164)(H,155,156)(H,157,158)(H,159,160)(H,161,162)(H,184,185)(H4,128,129,131)/t71-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,99-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-carboxy-2-[[(2S)-4-methyl-2-[[(2S)-3-methyl-2-[[(2S)-pyrrolidine-2-carbonyl]amino]butanoyl]amino]pentanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]hexanoic 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 and light. |
| 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: 12.5 mg/mL (4.77 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 | 0.3812 mL | 1.9061 mL | 3.8122 mL | |
| 5 mM | 0.0762 mL | 0.3812 mL | 0.7624 mL | |
| 10 mM | 0.0381 mL | 0.1906 mL | 0.3812 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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