| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Malantide targets PKA (cAMP-dependent protein kinase) as a highly specific substrate with a Km of 15 μM; it is also a substrate for PKC (protein kinase C), making it a versatile tool for studying kinase activity and signaling.
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|---|---|
| ln Vitro |
Malantide's Km values for PKA and PKG were 15 μM and 223 μM, in that order. PKA and PKG had respective Vmax values of 23.8 and 6.6 units/mg [1]. Only malantide showed statistically significant effects of isoproterenol on heart activity rate in guinea pigs [1].
In vitro kinase assays demonstrate that Malantide is a highly specific substrate for PKA with a Km of 15 μM; it shows >90% inhibition of substrate phosphorylation by protein kinase inhibitor (PKI) in various rat tissue extracts, confirming its specificity for PKA in complex biological samples. |
| ln Vivo |
In vivo studies using Malantide are typically conducted in tissue extracts or cell lysates rather than in live animals; the peptide is used to measure PKA activity in tissue samples, providing a readout of kinase activation in response to physiological or pharmacological stimuli.
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| Enzyme Assay |
The in vitro kinase assay for Malantide involves incubating the peptide substrate with purified PKA or PKC enzyme and [γ-32P]ATP, measuring the incorporation of radioactive phosphate into Malantide via scintillation counting or by phosphorimaging after SDS-PAGE; kinetic parameters (Km, Vmax) are determined from substrate concentration curves.
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| Cell Assay |
In vitro cell culture studies utilize cell lysates or permeabilized cells treated with Malantide and [γ-32P]ATP to measure PKA activity; alternatively, non-radioactive kinase assays using fluorescently labeled Malantide and detection by fluorescence polarization or time-resolved FRET are employed for high-throughput screening of kinase inhibitors.
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| Animal Protocol |
In vivo tissue extraction experiments involve harvesting tissues from animals following pharmacological treatments, preparing tissue lysates, and incubating with Malantide and [γ-32P]ATP to measure PKA activity; the degree of phosphorylation reflects the activation state of PKA in the tissue of interest.
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| ADME/Pharmacokinetics |
Malantide is a synthetic peptide with molecular weight 1633.89 g/mol; it is typically stored as a lyophilized powder at -20°C, reconstituted in aqueous buffers or DMSO, and stable under recommended storage conditions; solutions should be prepared fresh for kinase assays.
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| Toxicity/Toxicokinetics |
Toxicological data for Malantide are not applicable as it is a peptide substrate used in in vitro biochemical assays; the compound is not intended for therapeutic use, and standard laboratory safety precautions for handling peptides should be observed.
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| References |
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| Additional Infomation |
Malantide is a widely used research tool for studying PKA and PKC activity in biochemical and cell-based assays; its well-characterized kinetic properties make it valuable for comparative kinase activity studies, inhibitor screening, and signaling pathway analysis, though it is not approved for clinical use.
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| Molecular Formula |
C74H128N22O23
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|---|---|
| Molecular Weight |
1693.9417
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| Exact Mass |
1632.93
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| CAS # |
86555-35-3
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| Related CAS # |
Malantide TFA
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| PubChem CID |
135765
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| Appearance |
White to off-white solid powder
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| Density |
1.46g/cm3
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| Index of Refraction |
1.647
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| LogP |
1.661
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| Hydrogen Bond Donor Count |
25
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
55
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| Heavy Atom Count |
115
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| Complexity |
3250
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| Defined Atom Stereocenter Count |
15
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| SMILES |
CC[C@H](C)[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCN=C(N)N)N
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| InChi Key |
COABRICCWCYCPI-ZYLNUDMXSA-N
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| InChi Code |
InChI=1S/C72H124N22O21/c1-8-39(6)56(70(114)115)92-62(106)45(18-10-12-28-74)85-63(107)48(32-37(2)3)88-66(110)52-20-15-31-94(52)69(113)47(25-26-54(100)101)87-64(108)49(33-41-21-23-42(98)24-22-41)89-67(111)55(38(4)5)91-65(109)51(36-96)83-53(99)34-82-59(103)50(35-95)90-61(105)46(19-14-30-81-72(78)79)84-60(104)44(17-9-11-27-73)86-68(112)57(40(7)97)93-58(102)43(75)16-13-29-80-71(76)77/h21-24,37-40,43-52,55-57,95-98H,8-20,25-36,73-75H2,1-7H3,(H,82,103)(H,83,99)(H,84,104)(H,85,107)(H,86,112)(H,87,108)(H,88,110)(H,89,111)(H,90,105)(H,91,109)(H,92,106)(H,93,102)(H,100,101)(H,114,115)(H4,76,77,80)(H4,78,79,81)/t39-,40+,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,55-,56-,57-/m0/s1
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| Chemical Name |
(2S,3S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S,3R)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-3-methylpentanoic 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) |
DMSO : ~100 mg/mL (~61.20 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 | 0.5903 mL | 2.9517 mL | 5.9034 mL | |
| 5 mM | 0.1181 mL | 0.5903 mL | 1.1807 mL | |
| 10 mM | 0.0590 mL | 0.2952 mL | 0.5903 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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