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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
MIC: 0.125 mg/L (Pseudomonas aeruginosa Pa14) and 0.125 mg/L (Acinetobacter baumannii NCTC13301[1][2]
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ln Vitro |
Upleganan (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].
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ln Vivo |
In lung tissue and in the thigh model, Upleganan (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].
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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. |
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. |
Molecular Formula |
C52H82CLN15O12
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Molecular Weight |
1144.75
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CAS # |
2407717-17-1
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Related CAS # |
SPR206 acetate;2408422-41-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
ClC1=CC=CC(=C1)[C@@H](CN)CC(N[C@H](C(N[C@@H](CN)C(N[C@@H]1C(N[C@H](C(N[C@H](CC2C=CC=CC=2)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC1)=O)[C@@H](C)O)=O)CCN)=O)CCN)=O)CC(C)C)=O)=O)CCN)=O)=O)=O)[C@@H](C)O)=O
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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 | 0.8736 mL | 4.3678 mL | 8.7355 mL | |
5 mM | 0.1747 mL | 0.8736 mL | 1.7471 mL | |
10 mM | 0.0874 mL | 0.4368 mL | 0.8736 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.