| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| References | |
|---|---|
| Additional Infomation |
P-113D is a novel antimicrobial peptide drug composed of 12 amino acids, derived from histones, compounds naturally found in human saliva. Demegen is investigating it with the aim of developing it as a potential treatment for cystic fibrosis. A synthetic derivative of histone 5 has shown potential therapeutic activity in an experimental rat model of Pseudomonas aeruginosa sepsis.
Drug Indication It is used to treat cystic fibrosis and bacterial infections. Mechanism of Action P-113D inhibits their growth. Studies have shown that P-113D increases the permeability of the inner and outer membranes of Gram-negative bacteria by binding to the cell surface, thereby killing these bacteria within seconds. Pharmacodynamics P-113D has been shown to be active against conventional antibiotic-resistant bacteria clinically isolated from patients with cystic fibrosis (CF). The compound is stable and retains its activity in the sputum of CF patients. P-113D has been identified as the smallest histone fragment, and its antibacterial activity is comparable to that of the parent compound. Interestingly, P-113D can be obtained by synthesizing P113 from D-amino acids; this compound is not easily degraded by enzymes and retains the antibacterial activity of the parent compound. P-113D also exhibits very strong in vitro activity against a variety of Gram-negative and Gram-positive bacteria, including *Pseudomonas aeruginosa*, *Staphylococcus aureus*, *Haemophilus influenzae*, *Salmonella typhimurium*, *Escherichia coli*, *Staphylococcus epidermidis*, *Streptococcus mutans*, and *Streptococcus s.* P-113D has been shown to have antibacterial activity against a variety of clinical isolates from patients with cystic fibrosis (CF) who are resistant to conventional antibiotics, as well as P. aeruginosa and Staphylococcus aureus. P. aeruginosa isolates that produce thick alginate secretions (mucus phenotype) are also susceptible to P-113D's bactericidal activity. |
| Molecular Formula |
C71H110N28O13
|
|---|---|
| Molecular Weight |
1563.81
|
| Exact Mass |
1562.881
|
| CAS # |
348641-28-1
|
| Related CAS # |
P-113;190673-58-6
|
| PubChem CID |
71587612
|
| Sequence |
d-(Ala-Lys-Arg-His-His-Gly-Tyr-Lys-Arg-Lys-Phe-His)-NH2d-(AKRHHGYKRKFH)-NH2
|
| SequenceShortening |
d-(AKRHHGYKRKFH)-NH2
|
| Appearance |
Typically exists as solids at room temperature
|
| Hydrogen Bond Donor Count |
26
|
| Rotatable Bond Count |
55
|
| Heavy Atom Count |
112
|
| Complexity |
3000
|
| Defined Atom Stereocenter Count |
11
|
| SMILES |
C[C@H](C(=O)N[C@H](CCCCN)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CC1=CN=CN1)C(=O)N[C@H](CC2=CN=CN2)C(=O)NCC(=O)N[C@H](CC3=CC=C(C=C3)O)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC4=CC=CC=C4)C(=O)N[C@H](CC5=CN=CN5)C(=O)N)N
|
| InChi Key |
UIBPZXXSPHGPDS-UXLZJAPBSA-N
|
| InChi Code |
InChI=1S/C71H110N28O13/c1-41(75)60(103)91-48(15-5-8-24-72)62(105)94-52(19-12-28-85-71(79)80)66(109)99-57(33-46-36-83-40-89-46)69(112)98-56(32-45-35-82-39-88-45)61(104)86-37-58(101)90-54(30-43-20-22-47(100)23-21-43)67(110)95-49(16-6-9-25-73)63(106)93-51(18-11-27-84-70(77)78)64(107)92-50(17-7-10-26-74)65(108)97-55(29-42-13-3-2-4-14-42)68(111)96-53(59(76)102)31-44-34-81-38-87-44/h2-4,13-14,20-23,34-36,38-41,48-57,100H,5-12,15-19,24-33,37,72-75H2,1H3,(H2,76,102)(H,81,87)(H,82,88)(H,83,89)(H,86,104)(H,90,101)(H,91,103)(H,92,107)(H,93,106)(H,94,105)(H,95,110)(H,96,111)(H,97,108)(H,98,112)(H,99,109)(H4,77,78,84)(H4,79,80,85)/t41-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-/m1/s1
|
| Chemical Name |
(2R)-6-amino-N-[(2R)-1-[[(2R)-1-[[(2R)-1-[[2-[[(2R)-1-[[(2R)-6-amino-1-[[(2R)-1-[[(2R)-6-amino-1-[[(2R)-1-[[(2R)-1-amino-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]-2-[[(2R)-2-aminopropanoyl]amino]hexanamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.6395 mL | 3.1973 mL | 6.3946 mL | |
| 5 mM | 0.1279 mL | 0.6395 mL | 1.2789 mL | |
| 10 mM | 0.0639 mL | 0.3197 mL | 0.6395 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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