Quinotolast sodium (concentration range 1-100 μg/mL) inhibits histamine, LTC4 and PGD2 release in a concentration-dependent fashion.

Physicochemical Properties

Molecular Formula	C17H11N6NAO3
Molecular Weight	370.297413110733
Exact Mass	371.087
CAS #	101193-62-8
PubChem CID	14600474
Appearance	Light yellow to yellow solid powder
LogP	1.93
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	4
Heavy Atom Count	27
Complexity	726
Defined Atom Stereocenter Count	0
InChi Key	CDPWRMHFRRXOQH-UHFFFAOYSA-M
InChi Code	InChI=1S/C17H12N6O3.Na/c24-15(18-17-19-21-22-20-17)12-10-14(26-11-6-2-1-3-7-11)13-8-4-5-9-23(13)16(12)25;/h1-10H,(H2,18,19,20,21,22,24);/q;+1/p-1
Chemical Name	sodium;4-oxo-1-phenoxy-N-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)quinolizine-3-carboxamide
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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

ln Vitro	In dispersed human lung cells, quinotolast inhibits the release of histamine as well as the production of prostaglandin D2 and leukotriene (LT) C4. Quinotolast (100 μg/mL) markedly reduced PGD2 and LTC4 release. Quinotolast inhibits PGD2 release by 100% and LTC4 release by 54%. The inhibitory effect of quinotolast on histamine release from dispersed lung cells was largely independent of the preincubation period, and no tachyphylaxis was observed. Quinotolast has a significant inhibitory effect on inflammatory mediators in human dispersed lung cells [1]. Quinotolast also showed strong inhibitory effects on histamine and the peptide leukotrienes released from guinea pig lung fragments or mouse cultured mast cells. Quinotolast concentration-dependently inhibits pLT release from cultured mast cells. The IC50 value of Quinotolast is 0.72 μg/mL[2].
ln Vivo	Quinotolast can effectively suppress type I allergic reactions, including allergic bronchoconstriction and passive cutaneous anaphylaxis (PCA), in rats when administered intravenously and orally. When given intravenously to rats, quinotolast inhibits PCA in a dose-dependent manner. 0.0063 mg/kg of quinolast is the dose needed to suppress the response by 50% (ED50). When taken orally, quinotolast suppresses this reaction. Quinlilast's ED50 value is 0.0081 mg/kg. At a dose of 0.32 mg/kg, Quinotolast almost completely inhibited, but at a dose of 1 mg/kg, its effect was somewhat diminished [2].
References	[1]. Inhibition of histamine and eicosanoid release from dispersed human lung cells in vitro byquinotolast. Jpn J Pharmacol. 1995 Dec;69(4):375-80. [2]. Effects of quinotolast, a new orally active antiallergic drug, on experimental allergic models. Jpn J Pharmacol. 1993 Sep;63(1):73-81.

Solubility Data

Solubility (In Vitro)

DMSO : ~115 mg/mL (~309.71 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 5.75 mg/mL (15.49 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5.75 mg/mL (15.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.7005 mL	13.5026 mL	27.0051 mL
	5 mM	0.5401 mL	2.7005 mL	5.4010 mL
	10 mM	0.2701 mL	1.3503 mL	2.7005 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.