Bioactivity | Salcaprozate-d4 (sodium) is a deuterated labeled Salcaprozate (sodium)[1]. Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation[2][3]. |
Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注,因为它可能影响药物的药代动力学和代谢谱[1]。SNAC (12.5-400 μg/mL;24 h) 对 Caco-2 无细胞毒性,SNAC 为 200 μg/mL 时存活率在 90% 以上[4]。与 SAs 溶液的 Papp 相比,SNAC (50 和 200 μg/mL) 可将 RA 和 SA-B 的表观渗透系数 (Papp) 提高 2.14 倍和 3.68 倍[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Salcaprozate-d4 sodium 相关抗体: |
In Vivo | SNAC 改善 R1 和 SAs 的口服吸收并提高大鼠的生物利用度[4]。SNAC (2000 mg/kg/d;口服强饲 13 周) 相关的死亡率仅是明显的在 2000 毫克/公斤/天的水平下,男性为 20%,女性为 50%;没有明显的明确死因[2]。SNAC (100-1000 mg/kg/d;经口强饲 13 周) 在 Wistar 大鼠研究中剂量高达至 1000 mg/kg/天[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Formula | C15H16D4NNaO4 |
Molar Mass | 305.34 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Riley MGI, et, al. Subchronic oral toxicity of salcaprozate sodium (SNAC) in Sprague-Dawley and Wistar rats. Int J Toxicol. Jul-Aug 2009; 28(4):278-93. [3]. Twarog C, et, al. 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. [4]. Li Y, et, al. 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. |