Hi Marine, you can consider the following options depending on the solvents you have available. We generally recommend option 1 or 2 first. Please prepare freshly each time (do not store) and always include a solvent control.

1. 0.5% CMC-Na in saline, 5 mg/mL suspension

• Dissolve 0.5 g CMC-Na in saline. Heating at 60 °C water bath for several hours can help.
• Store at 4 °C for up to 1 week.
• Before use, warm at 37 °C and resuspend by sonication before dissolving the drug powder. Ensure a uniform suspension before injection

2. 50% PEG300 + 50% saline, 5 mg/mL solution

• Example: dissolve 1 mg compound in 500 µL PEG300, then add 500 µL saline.
• Use mild sonication or heating at 37 °C to fully dissolve.
• Administer immediately after preparation.

3. 15% Cremophor EL + 85% saline, 5 mg/mL solution

• Can also be aided by mild sonication or heating to achieve a uniform suspension.

The answer to this question is provided by MedChemExpress Technical Support.

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For your proposed study, a suitable solvent formulation for PKM2 inhibitor HY-103617 administered via tail vein injection to rats would likely consist of a mixture containing dimethyl sulfoxide (DMSO), polyethylene glycol (PEG), and saline. This combination is commonly used for intravenous delivery of poorly soluble small molecules in rodents, balancing solubility with acceptable toxicity for repeated dosing.

Recommended solvent formulation

Based on information from MedChemExpress and similar protocols, the following fresh formulation is a strong candidate:

• 10% DMSO
• 40% PEG300
• 5% Tween-80
• 45% Saline (0.9% NaCl in sterile water)

Formulation rationale

• DMSO: HY-103617 has limited solubility, and DMSO is an excellent organic solvent often used to achieve high stock solution concentrations. However, DMSO can be toxic, so its concentration in the final injection should be minimized. 10% is a common, well-tolerated percentage for intravenous use in rodents.
• PEG300: This is a biocompatible cosolvent frequently used in preclinical studies to enhance the solubility of hydrophobic compounds for intravenous administration.
• Tween-80: As a surfactant, Tween-80 (polysorbate 80) helps emulsify the drug, further improving its solubility and preventing precipitation upon contact with saline. A 5% concentration is generally considered safe for intravenous injection.
• Saline: Saline is the aqueous base for the formulation. It adjusts the tonicity and pH of the final solution to be more compatible with the blood, reducing the risk of hemolysis and injection site irritation.

Detailed preparation protocol

Important considerations

• Fresh preparation: For your 8-week study with repeated dosing, preparing the solution fresh for each injection is critical.
• Control group: An appropriate control group receiving only the solvent formulation (the vehicle) is essential to rule out any effects from the solvents themselves.
• Pilot study: Consider a small pilot study to test the tolerability of your chosen formulation in your rat model, monitoring for signs of toxicity or irritation, especially with a prolonged dosing schedule.