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10mg | ||
25mg | ||
50mg | ||
100mg | ||
250mg |
Purity: ≥98%
ABBV-4083, a Tylosin A analog with improvements in anti-Wolbachia and anti-filarial activity and oral pharmacokinetic properties, is a novel macrofilaricidal agent which acts by targeting the worm-symbiont Wolbachia bacterium. Chemical modification of TylA leads tos; ABBV-4083 has been selected for clinical evaluation.There is a significant need for improved treatments for onchocerciasis and lymphatic filariasis, diseases caused by filarial worm infection. In particular, an agent able to selectively kill adult worms (macrofilaricide) would be expected to substantially augment the benefits of mass drug administration (MDA) with current microfilaricides, and to provide a solution to treatment of onchocerciasis / loiasis co-infection, where MDA is restricted.
ln Vivo |
In recovered female adults, ABBV-4083 (150 mg/kg once daily for 14 days) decreased mouse Wolbachia levels by more than 99.9% (measured 16 weeks after therapy commencement, pti). Circulating microfilariae levels started to drop at 7 weeks after surgery and were totally eliminated from 12 weeks after surgery until the study's conclusion at 16 weeks [1].
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Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse or female gerbils are infected with Lactobacillus sigmodium larvae at 6-8 weeks of age through the bite of Bacchus mites [1].
Doses: 150 mg/kg. Doses: Oral administration starting at 14 weeks post-infection (pti), one time/day for 14 days. Experimental Results: Wolbachia levels (measured 16 weeks after the start of treatment, pti) were diminished by more than 99.9% in recovered female adults. Levels of circulating microfilariae diminished starting approximately 7 weeks postinoculation and were completely cleared from 12 weeks postinoculation to 16 weeks postinoculation at the end of this study. |
References |
[1]. von Geldern TW, et al. Discovery of ABBV-4083, a novel analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity. PLoS Negl Trop Dis. 2019 Feb 28;13(2):e0007159.
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Molecular Formula |
C53H82FNO17
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Molecular Weight |
1024.2131
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CAS # |
1809266-03-2
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Related CAS # |
1809266-03-2; 1401-69-0 (Tylosin A)
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SMILES |
O[C@@H]1[C@@H](C)O[C@](OC[C@H]([C@@H](CC)OC(C[C@H]([C@@H]([C@H]([C@@H](CC=O)C[C@H]2C)O[C@]3([H])O[C@H](C)[C@@H](O[C@]4([H])O[C@@H](C)[C@H](OCC5=CC=C(F)C=C5)[C@@](O)(C)C4)[C@H](N(C)C)[C@H]3O)C)O)=O)/C=C(C)/C=C/C2=O)([H])[C@H](OC)[C@@H]1OC
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Synonyms |
ABBV-4083; ABBV 4083; ABBV4083
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.9764 mL | 4.8818 mL | 9.7636 mL | |
5 mM | 0.1953 mL | 0.9764 mL | 1.9527 mL | |
10 mM | 0.0976 mL | 0.4882 mL | 0.9764 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.