| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Acetyl-Calpastatin (184-210) targets u-calpain with high potency, with a Ki value of 0.2 nM. It also inhibits cathepsin L with a Ki of 6 microM. The peptide does not inhibit papain or trypsin. Calpains are calcium-dependent cysteine proteases involved in various cellular processes.
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| ln Vitro |
In LCLC 103H cells, acetyl-calpastatin (184-210) (human) (Peptide 1; 12.5-100 μM) suppresses calpain with an IC50 of 27 μM [1].
In vitro, Acetyl-Calpastatin (184-210) potently inhibits calpain I (u-calpain) with a Ki of 0.2 nM. It also inhibits calpain II. The peptide shows selectivity for calpains over other proteases such as papain, trypsin, and cathepsin L (Ki = 6 microM). |
| ln Vivo |
In vivo, Acetyl-Calpastatin (184-210) is used to study the role of calpains in various physiological and pathological processes. Calpain inhibitors have potential therapeutic applications in conditions involving calcium-activated proteolysis, such as neurodegeneration, muscle wasting, and ischemia-reperfusion injury.
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| Enzyme Assay |
Enzyme assays for Acetyl-Calpastatin (184-210) involve incubating the peptide with purified calpain and a fluorogenic or chromogenic substrate. Calpain activity is measured by substrate cleavage, and inhibition is quantified by calculating Ki values from dose-response curves.
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| Cell Assay |
Cellular assays for Acetyl-Calpastatin (184-210) utilize cell lines or primary cells to assess calpain inhibition. Cells are treated with the peptide, and calpain activity is measured using cell-permeable fluorogenic substrates or by assessing calpain-mediated substrate cleavage by Western blot.
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| Animal Protocol |
In vivo studies with Acetyl-Calpastatin (184-210) are conducted in rodent models of calpain-related diseases. The peptide is typically administered via intraperitoneal or intravenous injection. Disease progression and calpain activity in tissues are assessed.
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| ADME/Pharmacokinetics |
As a 27-amino acid peptide, Acetyl-Calpastatin (184-210) is expected to have a short half-life due to proteolytic degradation. The acetyl modification at the N-terminus and amidation at the C-terminus provide some stability. The peptide should be stored at -20degC.
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| Toxicity/Toxicokinetics |
Toxicity data for Acetyl-Calpastatin (184-210) are limited. Calpain inhibitors are generally well-tolerated, but chronic inhibition may have effects on normal cellular functions. Standard safety precautions for laboratory handling of peptides should be followed.
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| References | |
| Additional Infomation |
Caloplasm inhibitor Ac 184-210 is a 27-amino acid polypeptide with the sequence Ac-Asp-Pro-Met-Ser-Ser-Thr-Tyr-Ile-Glu-Glu-Leu-Gly-Lys-Arg-Glu-Val-Thr-Ile-Pro-Pro-Lys-Tyr-Arg-Glu-Leu-Leu-Ala-NH2. It is an acetylated synthetic peptide of human calpains inhibitory peptide, potently inhibiting calpains I and II, but without inhibitory activity against papain (a cysteine protease) or trypsin (a serine protease). It functions as an inhibitor of EC 3.4.22.52 (calpains-1) and EC 3.4.22.53 (calpains-2).
Acetyl-Calpastatin (184-210) is a research-use peptide and is not approved for therapeutic applications. It is also known as Calpastatin Peptide B27-WT. The peptide is used to study calpain function in various biological processes and diseases. It is available from multiple research suppliers. |
| Molecular Formula |
C142H230N36O44S
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|---|---|
| Molecular Weight |
3177.63000
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| Exact Mass |
3175.66
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| CAS # |
123714-50-1
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| Related CAS # |
Acetyl-Calpastatin(184-210)(human) TFA
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| PubChem CID |
90488788
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| Appearance |
White to off-white solid powder
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| LogP |
3.43
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| Hydrogen Bond Donor Count |
44
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| Hydrogen Bond Acceptor Count |
49
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| Rotatable Bond Count |
105
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| Heavy Atom Count |
223
|
| Complexity |
7290
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| Defined Atom Stereocenter Count |
30
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1CCC[C@H]1C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCSC)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CC(=O)O)NC(=O)C
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| InChi Key |
ZXJCOYBPXOBJMU-HSQGJUDPSA-N
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| InChi Code |
InChI=1S/C142H230N36O44S/c1-18-74(11)111(172-129(211)97(65-81-38-42-83(185)43-39-81)168-136(218)113(77(14)181)174-131(213)100(69-180)170-130(212)99(68-179)169-124(206)92(52-60-223-17)162-132(214)101-33-26-57-176(101)138(220)98(66-109(195)196)154-79(16)183)135(217)163-90(46-50-107(191)192)121(203)159-88(44-48-105(187)188)122(204)164-93(61-70(3)4)116(198)152-67-104(186)155-84(29-20-22-53-143)117(199)156-86(31-24-55-150-141(146)147)118(200)160-91(47-51-108(193)194)125(207)171-110(73(9)10)134(216)175-114(78(15)182)137(219)173-112(75(12)19-2)140(222)178-59-28-35-103(178)139(221)177-58-27-34-102(177)133(215)161-85(30-21-23-54-144)120(202)167-96(64-80-36-40-82(184)41-37-80)128(210)157-87(32-25-56-151-142(148)149)119(201)158-89(45-49-106(189)190)123(205)165-95(63-72(7)8)127(209)166-94(62-71(5)6)126(208)153-76(13)115(145)197/h36-43,70-78,84-103,110-114,179-182,184-185H,18-35,44-69,143-144H2,1-17H3,(H2,145,197)(H,152,198)(H,153,208)(H,154,183)(H,155,186)(H,156,199)(H,157,210)(H,158,201)(H,159,203)(H,160,200)(H,161,215)(H,162,214)(H,163,217)(H,164,204)(H,165,205)(H,166,209)(H,167,202)(H,168,218)(H,169,206)(H,170,212)(H,171,207)(H,172,211)(H,173,219)(H,174,213)(H,175,216)(H,187,188)(H,189,190)(H,191,192)(H,193,194)(H,195,196)(H4,146,147,150)(H4,148,149,151)/t74-,75-,76-,77+,78+,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,110-,111-,112-,113-,114-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-1-[(2S,3S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-carboxypropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-6-aminohexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-6-aminohexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]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 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) |
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 | 0.3147 mL | 1.5735 mL | 3.1470 mL | |
| 5 mM | 0.0629 mL | 0.3147 mL | 0.6294 mL | |
| 10 mM | 0.0315 mL | 0.1574 mL | 0.3147 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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