| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Gamma-aminobutyric acid (GABA) receptors, specifically the benzodiazepine site of the GABAA receptor. alpha-Casozepine binds to the benzodiazepine site of the GABAA receptor with an IC50 of 88 µM in bovine samples. This binding modulates GABAergic neurotransmission, contributing to its anxiolytic effects.
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| ln Vitro |
alpha-Casozepine exhibits affinity for GABA receptors in vitro, with an IC50 of 88 µM at the benzodiazepine site of the GABAA receptor in bovine samples. The peptide has been shown to modulate GABA-induced chloride conductance and enhance pentobarbital-induced sleep in experimental models. Its bioactivity has been characterized in various receptor binding and functional assays.
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| ln Vivo |
In vivo, alpha-Casozepine demonstrates anti-anxiety effects in animal models. It has been shown to enhance pentobarbital-induced sleep in mice via the GABAA receptor. The peptide is orally effective as an anxiolytic agent. Its effects on anxiety-related behaviors have been evaluated in various behavioral paradigms, including elevated plus maze and open field tests.
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| Enzyme Assay |
In vitro receptor binding assays for alpha-Casozepine typically involve competition binding experiments using radiolabeled ligands such as [3H]-flunitrazepam for the benzodiazepine site of the GABAA receptor. Membranes are prepared from bovine brain or cells expressing GABAA receptors. The peptide is incubated at varying concentrations, and bound radioactivity is measured. IC50 values are calculated from displacement curves. Functional assays may also measure GABA-induced chloride conductance.
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| Cell Assay |
In vitro cell-based assays for alpha-Casozepine are not extensively documented. When performed, they typically involve cells expressing GABAA receptors, such as Xenopus laevis oocytes or mammalian cell lines. The peptide's ability to modulate GABA-induced currents is assessed using electrophysiological techniques. Cells are cultured in appropriate media and treated with alpha-Casozepine prior to or during GABA application.
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| Animal Protocol |
In vivo animal studies for alpha-Casozepine have been conducted in mice to evaluate its anxiolytic and sedative effects. The peptide is typically administered orally or intraperitoneally. The elevated plus maze, open field test, and pentobarbital-induced sleep assay are commonly used to assess anxiety-related behaviors and sedation. Dosing regimens vary, but the compound has been shown to be effective at doses that produce behavioral changes.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for alpha-Casozepine are limited. The peptide is soluble in DMSO (15 mg/mL) and water (50 mg/mL when pH is adjusted to 2 with 1 M HCl). It should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 1 year. Its molecular weight is 1267.47. Detailed ADME parameters are not publicly available.
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| Toxicity/Toxicokinetics |
alpha-Casozepine is generally considered safe for research use. It is a bioactive peptide derived from milk and is not known to be toxic at research-relevant concentrations. However, comprehensive toxicological data are not available. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety precautions should be taken when handling the peptide.
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| Additional Infomation |
alpha-Casozepine is a bioactive decapeptide derived from bovine alpha-S1 casein. It acts as an anxiolytic by binding to the benzodiazepine site of the GABAA receptor with an IC50 of 88 µM. The peptide is also known by the synonym Lactium. It has been studied for its potential applications in anxiety and sleep disorders. The compound is not approved for clinical use and is available only for research purposes.
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| Molecular Formula |
C60H94N14O16
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|---|---|
| Molecular Weight |
1267.47
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| Exact Mass |
1266.697
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| CAS # |
117592-45-7
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| PubChem CID |
10351433
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| Appearance |
White to off-white solid powder
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| LogP |
-0.8
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| Hydrogen Bond Donor Count |
17
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
41
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| Heavy Atom Count |
90
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| Complexity |
2410
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CC=C(C=C1)O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC2=CC=C(C=C2)O)N
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| InChi Key |
SKGURMFKEAFAGD-CSYZDTNESA-N
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| InChi Code |
InChI=1S/C60H94N14O16/c1-31(2)24-43(71-51(81)39(61)28-35-11-15-37(75)16-12-35)52(82)66-30-49(78)67-47(29-36-13-17-38(76)18-14-36)58(88)74-44(25-32(3)4)55(85)69-41(20-22-50(79)80)53(83)68-40(19-21-48(62)77)54(84)72-46(27-34(7)8)57(87)73-45(26-33(5)6)56(86)70-42(59(89)90)10-9-23-65-60(63)64/h11-18,31-34,39-47,75-76H,9-10,19-30,61H2,1-8H3,(H2,62,77)(H,66,82)(H,67,78)(H,68,83)(H,69,85)(H,70,86)(H,71,81)(H,72,84)(H,73,87)(H,74,88)(H,79,80)(H,89,90)(H4,63,64,65)/t39-,40-,41-,42-,43-,44-,45-,46-,47-/m0/s1
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| Chemical Name |
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxy-4-(diaminomethylideneamino)butyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoic 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.7890 mL | 3.9449 mL | 7.8897 mL | |
| 5 mM | 0.1578 mL | 0.7890 mL | 1.5779 mL | |
| 10 mM | 0.0789 mL | 0.3945 mL | 0.7890 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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