Salcaprozate sodium (SNAC) is an oral absorption enhancer with potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium increases passive transcellular penetration of small intestinal epithelial cells by increasing lipophilicity due to non-covalent macromolecular complexation.

Physicochemical Properties

Molecular Formula	C15H20NNAO4
Molecular Weight	301.31
Exact Mass	301.128
CAS #	203787-91-1
PubChem CID	23669833
Appearance	White to off-white solid powder
Boiling Point	521.7ºC at 760 mmHg
Flash Point	269.3ºC
Vapour Pressure	1.03E-11mmHg at 25°C
LogP	1.603
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	9
Heavy Atom Count	21
Complexity	312
Defined Atom Stereocenter Count	0
InChi Key	UOENJXXSKABLJL-UHFFFAOYSA-M
InChi Code	InChI=1S/C15H21NO4.Na/c17-13-9-6-5-8-12(13)15(20)16-11-7-3-1-2-4-10-14(18)19;/h5-6,8-9,17H,1-4,7,10-11H2,(H,16,20)(H,18,19);/q;+1/p-1
Chemical Name	sodium;8-[(2-hydroxybenzoyl)amino]octanoate
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	When SNAC is at 200 μg/mL, the survival rate is over 90% and it has no cytotoxicity against Caco-2 (12.5-400 μg/mL; 24 h) [3]. The apparent permeability coefficient (Papp) of RA and SA-B can be increased by 2.14 and 3.68 times, respectively, by SNAC (50 and 200 μg/mL) in comparison to Papp of SAs solution [3].
ln Vivo	In rats, SNAC enhances R1 and SAs' oral absorption and raises their bioavailability[3]. Only 20% of men and 50% of women died from SNAC (2000 mg/kg/d; oral gavage for 13 weeks)-related deaths, with no obvious reason given for the deaths[1]. Wistar rats were given oral gavage of SNAC at a dose of up to 1000 mg/kg/day for 13 weeks[1].
Animal Protocol	Animal/Disease Models: SD (Sprague-Dawley) rats (6-7 weeks)[1] Doses: 2000 mg/kg/d Route of Administration: po (oral gavage) for 13 weeks Experimental Results: Induced 20% and 50% mortality in males and females at the dose of 2000 mg /kg/d.
References	[1]. Subchronic oral toxicity of salcaprozate sodium (SNAC) in Sprague-Dawley and Wistar rats. Int J Toxicol. Jul-Aug 2009; 28(4):278-93. [2]. Intestinal Permeation Enhancers for Oral Delivery of Macromolecules: A Comparison between Salcaprozate Sodium (SNAC) and Sodium Caprate (C 10). Pharmaceutics. 2019 Feb 13; 11(2):78. [3]. Impact of Sodium N-[8-(2-Hydroxybenzoyl)amino]-caprylate on Intestinal Permeability for Notoginsenoside R1 and Salvianolic Acids in Caco-2 Cells Transport and Rat Pharmacokinetics. Molecules. 2018 Nov 16; 23(11):2990.
Additional Infomation	Salcaprozate Sodium is the sodium salt form of salcaprozate, an oral absorption promoter. Salcaprozate sodium may be used as a delivery agent to promote the oral absorption of certain macromolecules with poor bioavailability such as insulin and heparin.

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (165.94 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (8.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 25.0 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: ≥ 2.5 mg/mL (8.30 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 25.0 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (8.30 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.3188 mL	16.5942 mL	33.1884 mL
	5 mM	0.6638 mL	3.3188 mL	6.6377 mL
	10 mM	0.3319 mL	1.6594 mL	3.3188 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.