| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
MIC: 0.125 mg/L (Pseudomonas aeruginosa Pa14) and 0.125 mg/L (Acinetobacter baumannii NCTC13301)[1][2]
Bacterial outer membrane of Gram-negative pathogens. |
|---|---|
| ln Vitro |
SPR206 demonstrates significant antimicrobial activity against bacteria that are Gram-negative. SPR206 has decreased cytotoxicity with MIC values of 8 mg/L, 0.125 mg/L, 0.125 mg/L, 0.25 mg/L, 0.06 mg/L, and 0.125 mg/L against E. coli IHMA558090, E. coli ATCC 25922, K. pneumonia ATCC 13882, P. aeruginosa ATCC 27853, and A. baumannii ATCC 19003 [1].
SPR206 acetate demonstrates significant antimicrobial activity against Gram-negative bacteria. It shows potent activity against Pseudomonas aeruginosa strain Pa14 and Acinetobacter baumannii strain NCTC13301, with MIC values of 0.125 mg/L for both strains. It displays MIC values of 8 mg/L for E. coli. |
| ln Vivo |
In lung tissue and in the thigh model, SPR206 (0.125-30 mg/kg; intravenous injection or subcutaneous injection; every 8 hours or every 4 hours; for 16 hours or 24 hours; neutropenic mice) therapy decreases the burden of Pa14 and NCTC13301[2].
Not available in the public domain. As a polymyxin analog, its in vivo efficacy would typically be evaluated in mouse models of infection, where it is administered to assess its ability to reduce bacterial burden and improve survival against MDR Gram-negative pathogens. |
| Enzyme Assay |
The antimicrobial activity is assessed by determining the Minimum Inhibitory Concentration (MIC) using the broth microdilution method according to CLSI guidelines. A panel of Gram-negative bacterial strains, including MDR clinical isolates, is tested.
|
| Cell Assay |
Cell viability assays are performed against a panel of Gram-negative bacteria. The minimum bactericidal concentration (MBC) can also be determined to assess the compound's bactericidal activity.
|
| Animal Protocol |
Animal/Disease Models: Neutropenic mice infected Pa14 or NCTC13301[2]
Doses: 3 mg/kg, 10 mg/kg, 20 mg/kg, 30 mg/kg (intravenous (iv)injection); 0.125 mg/kg, 0.5 mg/kg, 1 mg/kg, 4 mg/kg (subcutaneous (sc)injection) Route of Administration: intravenous (iv)injection or subcutaneous (sc)injection; every 8 hrs (hours) or every 4 hrs (hours); for 16 hrs (hours) or 24 hrs (hours) Experimental Results: In lung tissue, diminished the burden of Pa14 and NCTC13301 by 1.5 and 3.6 log10 CFU/mL. In the thigh model, diminished the burden of Ab13301 by 3.4 and 4.3 log10 CFU/g. |
| ADME/Pharmacokinetics |
Physicochemical properties: SPR206 acetate is a polymyxin analog. Its solubility and stability are optimized for in vivo administration. Storage: Typically stored at -20degC.
|
| References |
[1]. Brown P, et al. Design of Next Generation Polymyxins with Lower Toxicity: The Discovery of SPR206. ACS Infect Dis. 2019 Oct 11;5(10):1645-1656.
[2]. L. Grosser, et al. In Vivo Efficacy of SPR206 in Murine Lung and Thigh Infection Models Caused by Multidrug Resistant Pathogens Pseudomonas aeruginosa and Acinetobacter baumanii. Poster-139 ASM ESCMID 2018 Lisbon, Portugal. [3]. Noushin Akhoundsadegh, et al. Outer Membrane Interaction Kinetics of New Polymyxin B Analogs in Gram-Negative Bacilli. Antimicrob Agents Chemother. 2019 Sep 23;63(10):e00935-19. |
| Additional Infomation |
SPR206 acetate (CAS#: 2408422-41-1) is a next-generation polymyxin antibiotic developed to address the growing threat of antimicrobial resistance. It is designed to retain the potent activity of polymyxins against Gram-negative bacteria while potentially improving its safety profile. It is a promising candidate for treating infections caused by MDR pathogens.
|
| Molecular Formula |
C54H86CLN15O14
|
|---|---|
| Molecular Weight |
1204.8057513237
|
| Exact Mass |
1203.616
|
| CAS # |
2408422-41-1
|
| Related CAS # |
Upleganan;2407717-17-1
|
| PubChem CID |
165412291
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
18
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
22
|
| Heavy Atom Count |
84
|
| Complexity |
2090
|
| Defined Atom Stereocenter Count |
12
|
| SMILES |
C[C@H]([C@H]1C(=O)NCC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCN)CCN)CC(C)C)CC2=CC=CC=C2)CCN)NC(=O)[C@H](CN)NC(=O)[C@H]([C@@H](C)O)NC(=O)C[C@H](CN)C3=CC(=CC=C3)Cl)O.CC(=O)O
|
| InChi Key |
YADKGXKKBAFXFJ-CYMYEOQJSA-N
|
| InChi Code |
InChI=1S/C52H82ClN15O12.C2H4O2/c1-27(2)21-38-48(76)62-34(13-17-54)44(72)61-36(15-19-56)47(75)68-42(28(3)69)51(79)59-20-16-37(46(74)60-35(14-18-55)45(73)65-39(49(77)64-38)22-30-9-6-5-7-10-30)63-50(78)40(26-58)66-52(80)43(29(4)70)67-41(71)24-32(25-57)31-11-8-12-33(53)23-31;1-2(3)4/h5-12,23,27-29,32,34-40,42-43,69-70H,13-22,24-26,54-58H2,1-4H3,(H,59,79)(H,60,74)(H,61,72)(H,62,76)(H,63,78)(H,64,77)(H,65,73)(H,66,80)(H,67,71)(H,68,75);1H3,(H,3,4)/t28-,29-,32-,34+,35+,36+,37+,38+,39-,40+,42+,43+;/m1./s1
|
| Chemical Name |
acetic acid;(2S,3R)-2-[[(3S)-4-amino-3-(3-chlorophenyl)butanoyl]amino]-N-[(2S)-3-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]propan-2-yl]-3-hydroxybutanamide
|
| 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 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)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8300 mL | 4.1500 mL | 8.3001 mL | |
| 5 mM | 0.1660 mL | 0.8300 mL | 1.6600 mL | |
| 10 mM | 0.0830 mL | 0.4150 mL | 0.8300 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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