(S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly effective H1 receptor antagonist. (S)-Setastine has a long-lasting antihistamine effect and good oral efficacy. (S)-Setastine can be used in the research of allergic diseases.

Physicochemical Properties

Molecular Formula	C22H28CLNO
Molecular Weight	357.92
Appearance	White to off-white solid powder
Synonyms	(S)-EGIS-2062 free acid; (S)-EGYT-2062 free acid
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
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Porszasz J, et al. Pharmacology of the new H1-receptor antagonist setastine hydrochloride[J]. Arzneimittel-forschung, 1990, 40(12): 1340-1345.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~279.39 mM; with ultrasonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 5 mg/mL (13.97 mM) (saturation unknown) in 10% DMSO +40% PEG300 +5% Tween-80 +45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution。 Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (13.97 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 the 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD in saline and mix well. 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. Solubility in Formulation 3: ≥ 5 mg/mL (13.97 mM) (saturation unknown) in 10% DMSO +90% Corn Oil (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 the 50.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well. " (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.7939 mL	13.9696 mL	27.9392 mL
	5 mM	0.5588 mL	2.7939 mL	5.5878 mL
	10 mM	0.2794 mL	1.3970 mL	2.7939 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.