The oligonucleotide synthesis services at Aurigene is supported by a state-of-the-art lab facility and skilled scientists with expertise in various types of oligos. We have an in-house custom synthesis of phosphoramidites and the ability to perform complex conjugation using click chemistry, amide coupling and thiol mediated C-S & S-S bond.
Our dedicated lab space of 1000 sq.ft is equipped with humidity control. Aurigene’s oligonucleotide platform is supported by trained team that helps optimize the designed oligonucleotide along with primary assay iterations. We have the ability to synthesize 10-40-mer oligonucleotide up to 1-gram scale. We perform all standard modifications, with or without backbone modification, for which phosphoramidites are made in-house and also available commercially. Oligo equipments at Aurigene: K and A H-16 automated DNA/RNA synthesizer AKTA pure 25M FPLC purification system Sartoflow smart TFF system for concentration and desalting Martin Christ LSC plus lyophilizer with lyocube, benchtop tray lyophilizer Agilent LC-MS for oligonucleotide analysis Implen N60 nano spectrophotometer
Synthesis and Purification
- Scale: 1-100 µmol (1-100 mg)
- 16x1 µmol, 4x20 µmol, 1x100 µmol
- Size: 10 to 40-mer
- 2’-F, 2’-OMe, 2’-O-MOE, LNA and all standard modifications
- Anion/ Cation exchange purification
- Reverse phase HPLC
- Size exclusion
- Desalting
Analysis
- UV quantification
- Purity and identity analysis using LC-MS (TOF) and mass deconvolution
- HPLC with different mobile and stationary phase for purity assessment
Biology
- In vitro IC50, Kd and binding assessment and in vivo activities evaluation with wide range of cells. Efficacy experiment in oncology and inflammation model
- Toxicology studies with ASO.
Conjugation
- Acid-amine coupling
- Alkyne-azide coupling
- Thiol-maleimide coupling
- S-S and C-S bond formation
Why Aurigene Pharmaceutical Services?
Complex conjugation using click chemistry, amide coupling and thiol mediated C-S & S-S bond
Ion exchange and reverse phase HPLC
Expertise in nucleoside, sugar modifications, base modifications
State-of-the-art drug discovery facility using oligonucleotide modality
CADD Optimization
Synthesis between 10-40-mer oligonucleotide
In-house custom phosphoramidite synthesis
Integrated Services
Virtual Tour
Hyderabad R and D Center
Bangalore R and D Center
Oligo
Resources
JULY 02, 2021
Oligonucleotide as a novel class of therapeutic modality
Oligonucleotides as a therapeutic class is a revolutionary approach to discover new and important therapeutic agents for treating human diseases. RNA-based intervention at times works in cases where other modalities do not work. For example, it may help in treating inborn errors in metabolism, genetic disorders and rareOligonucleotide therapeutics is the use of c...
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HPAPI Molecule from Development to Market
The global Highly Potent Active Pharmaceutical Ingredients (HPAPI) market is expected to reach USD 26.84 Billion by 2023 from USD 17.72 Billion in 2018, at a CAGR 8.7%....
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cGMP Development and Manufacturing Services
Aurigene Pharmaceutical Services has a legacy of +20 years in developing and manufacturing compounds under cGMP. Our manufacturing plants are spread across 3 continents with facilities in India, UK, and Mexico. ...
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Developing a methodology for In situ perfusion based combined tissue distribution and toxicity evaluation study
Challenges: Several repeated in house validation studies were performed to optimize the suitable perfusate (liquid medium intended to pass through the heart), perfusate volume and perfusion rate to ensure complete perfusion of animal subjects (parameters weren’t adjustable) Challenges were encountered in adjusting the perfusion volume and rate vis-à-vis ensuri...
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Synthesis of 2-hydroxy-3-alkyl-2-phenyl-2,3- dihydroquinazolin-4(1H)-one via molybdenum hexacarbonyl mediated CO gas- and ligand free carbonylative reactions
2016
Carbon monoxide gas and ligand-free conditions were developed for the synthesis of 2-hydroxy-3-alkyl-2-phenyl-2,3-dihydroquinazolin4(1H)-one via catalytic carbonylation with molybdenum hexacarbonyl as an efficient carbonylating agent for the three-component reaction of isatoic anhydride, amine, iodobenzene. Mo(CO)6 is a solid carbon monoxide source. The quinazoli...
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Alternate end-game strategies towards Nirmatrelvir synthesis: Defining a continuous flow process for the preparation of an anti-COVID drug
2005
Scalable alternate end-game strategies for the synthesis of the anti-COVID drug molecule Nirmatrelvir (1,PF-07321332) have been described. The first involves a direct synthesis of 1 via amidation of the carboxylic acid 7 (suitably activated as a mixed anhydride with either pivaloyl chloride or T3P) with the ...
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Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
2005
Mutations in MEK1/2 have been described as a resistance mechanism to BRAF/MEK inhibitor treatment. We report the discovery of a novel ATP-competitive MEK1/2 inhibitor with efficacy in wildtype (WT) and mutant MEK12 models. Starting from a HTS hit, we obtained selective, cellularly active ...
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Synthesis of Anti-covid Drug Nirmatrelvir Using Flow Chemistry
2005
Synthesis of the anti-covid therapeutic Nirmatrelvir by using flow chemistry to enhance efficiency of amide to nitrile conversion in a functionally and Stereochemically Embellished environment. ...
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Frequently asked questions
How are oligonucleotides synthesized?
Oligonucleotides can be synthesized using solid-phase (Peptides) and one pot liquid phase (enzymatic) method in the lab for milligram to multi-kilogram scale. Steps involved in solid-phase Oligo synthesis are detritylation, coupling, oxidation and capping. One-pot liquid phase oligo synthesis requires polymerase enzyme, template oligonucleotide and nucleotide triphosphate as starting materials.
How accuracy of chemical synthesis of oligonucleotides is maintained?
Accuracy of chemical synthesis of Oligonucleotides is maintained by maintaining the order of starting materials used during the synthesis process.
What are oligonucleotide drugs?
Oligonucleotide drugs help modulate the effect of a disease-causing gene by targeted degradation/activation of gene expression or gene editing. This activity may cause the disease to be controlled or cured.
How stable are the Oligos?
Oligos are stable for 6 weeks in buffer when stored at 37°C and for long-term stability is to be stored between -20°C to -80°C. During storage, oligos should not be exposed to direct sunlight or UV rays.
What is the oligo synthesis scale?
We can Synthesis 10-40-mer oligonucleotide up to 1 gram scale.
Can you incorporate a specific modification into Oligo?
We can perform all standard modifications, with or without backbone modification, for which Phosphoramidites are commercially available. We also have the capabilities of making any customized Phosphoramidite in-house.
What are the recommended storage conditions for Oligonucleotides?
For a period of 6 weeks, Oligos can be stored in T10E1 buffer at 37°C and for the long term, Oligonucleotides can be dried down and stored with or without TE buffer at -20°C.
Does Oligonucleotide have a phosphate on the 5’ or 3’ end?
Typical Oligonucleotide synthesis does not produce phosphate on the 5’ or 3’ end. On request, oligonucleotides can be synthesized with phosphate on the 5’ or 3’ end.
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