Ulinastatin (Uristatin) is a trypsin and serine protease inhibitor. Ulinastatin is a major protein-binding inhibitor of several trypsins, chymotrypsin, and several pancreatic proteases. Ulinastatin has neuro-protection, anti-inflammatory, anti-apoptotic, and antioxidant effects.

Physicochemical Properties

Molecular Formula	C13H16O3
Molecular Weight	220.264344215393
Exact Mass	220.109
CAS #	80449-31-6
Appearance	White to off-white solid powder
Density	1.2±0.1 g/cm3
Boiling Point	331.5±42.0 °C at 760 mmHg
Flash Point	171.0±16.8 °C
Vapour Pressure	0.0±0.7 mmHg at 25°C
Index of Refraction	1.549
LogP	2.87
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: This product requires protection from light (avoid light exposure) during transportation and storage.
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 LPS-stimulated BEAS-2B cells, urinastatin (500–5000 U; 24 hours) can drastically reduce TLR4 expression and NF-κB activation [1]. Linstatin
ln Vivo	Animals exposed to LPS-induced acute lung injury (ALI) were significantly protected by ulinstatin (10000 U/kg; intravenous injection; twice); this was achieved by lowering lung wet/dry weight ratio, ALI score, total cells, neutrophils, macrophages, myeloperoxidase activity, and malondialdehyde content—factors linked to lung histological damage [1].
Cell Assay	Western Blot Analysis[1] Cell Types: Human lung epithelial BEAS-2B cells Tested Concentrations: 500 U, 2500 U, 5000 U Incubation Duration: 24 hrs (hours) Experimental Results: Markedly attenuated TLR4 expression and NF-κB activation in LPS-stimulated BEAS-2B cells.
Animal Protocol	Animal/Disease Models: Male C57BL/6 mice (8-10 weeks old, 18-22 g)[1] Doses: 10000 U/kg Route of Administration: iv; twice (1 h before and 6 h after LPS treatment) Experimental Results: Dramatically protected animals from LPS-induced ALI.
References	[1]. Research progress of ulinastatin in the treatment of liver diseases. Int J Clin Exp Pathol. 2020 Nov 1;13(11):2720-2726. [2]. Ulinastatin Protects Against LPS-Induced Acute Lung Injury By Attenuating TLR4/NF-κB Pathway Activation and Reducing Inflammatory Mediators. Shock. 2018 Nov;50(5):595-605.

Solubility Data

Solubility (In Vitro)

H2O : ~10 mg/mL DMSO : ~1 mg/mL

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.5401 mL	22.7004 mL	45.4009 mL
	5 mM	0.9080 mL	4.5401 mL	9.0802 mL
	10 mM	0.4540 mL	2.2700 mL	4.5401 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.