Low molecular weight protamine acetate  (Synonyms: LMWP acetate; TDSP5 acetate)

Low molecular weight protamine (LMWP) is a truncated arginine-rich protamine peptide, which also acts as an antidote for heparin/low molecular weight heparin and a cell-penetrating delivery vector. Low molecular weight protamine neutralizes heparin-induced anticoagulant activities, including aPTT, anti-Xa and anti-IIa activities. Low molecular weight protamine translocates across mammalian cell membranes, delivers conjugated impermeable molecules through tumor tissues, enhances the skin permeability of conjugated epidermal growth factor, and accelerates wound healing when conjugated with epidermal growth factor. Low molecular weight protamine retains the in vitro cell proliferation activity of conjugated EGF, and also enables site-specific conjugation with peptides or proteins via genetic recombination. Low molecular weight protamine can be used in studies related to colon cancer, skin wounds and diabetic skin wounds^[1][2][3].

Low molecular weight protamine (LMWP) (18 μg/U; 3 min) 可在 18 μg/U 的比例下完全中和人血浆中 5 U/mL 肝素的 aPTT 活性，所需剂量比鱼精蛋白高约 2.4 倍^[1]。
Low molecular weight protamine (LMWP) (12 μg/U; 10 min) 可在人血浆中以 12 μg/U 的比例完全中和 1 U/mL 肝素的抗 IIa 活性，所需剂量比鱼精蛋白高约 1.6 倍^[1]。
Low molecular weight protamine (LMWP) (30 μg/μg) 可完全中和 Mono-Embolex 的抗 Xa 活性，二者比例为 30 μg/μg，效力与鱼精蛋白相似^[1]。
Low molecular weight protamine (LMWP) (100 μg/U) 可完全中和 Fragmin 和 LMWH3000 的抗 Xa 因子活性，中和比例为 100 μg/U，表明其对低分子肝素具有广泛的效用^[1]。
Low molecular weight protamine (LMWP) (4.5 mg/mL; 60 min at 37°C) 在稀释的人血清中仅诱导 30%的补体消耗，与鱼精蛋白相比，其补体激活潜能显著降低^[1]。
Heparin-Low molecular weight protamine (LMWP) 复合物 (22 μg/U; 60 min at 37°C)，以 22 μg/U 的比例形成，在含 2.5-10 U/mL heparin 的人血清中仅诱导约 50%的补体消耗，与肝素-鱼精蛋白复合物相比显示出更低的补体激活潜能^[1]。
Low molecular weight protamine (LMWP) (63 μM; 2 h at 37°C) 可与小鼠抗鱼精蛋白抗体发生交叉反应，其 IC₅₀ 为 63 μM，交叉反应性较鱼精蛋白低约 5.25 倍^[1]。
Low molecular weight protamine (LMWP)-gelonin 偶联物可在无细胞兔网织红细胞裂解液体系中强效抑制蛋白质合成，其 IC₅₀ 约为 23 pM^[2]。
FITC-labeled Low molecular weight protamine (LMWP) (TDSP5) (0.2 μM; 30 min) 可被 293T、HeLa、CT-26、MCF-7、NIH3T3 和 MG63 细胞高效摄取，摄取效率与 TAT 肽及鱼精蛋白相当，且不受 10%血清的影响^[2]。
Low molecular weight protamine (LMWP) (TDSP5) (0.2 μM; 30 min) 可高效转位至 HeLa、CT-26 和 MG63 细胞内，定位于细胞质，并且能有效将偶联的鬼笔环肽和皂草素递送至细胞中^[2]。
Low molecular weight protamine (LMWP) (TDSP5) (0.01-10.0 mM; 72 h) 对 293T 细胞表现出极低的细胞毒性，在 10.0 mM 的最高浓度下孵育 72 h 后，细胞活力下降不足 10%^[2]。
Low molecular weight protamine (LMWP)-gelonin 偶联物 (摩尔比 1:1)(孵育 48 h) 可强效抑制 CT-26 结肠腺癌细胞的生长，孵育 48 h 后的 IC₅₀ 为 39 pM，而游离 gelonin 或游离 LMWP 与 gelonin 的混合物则无此作用^[2]。
Low molecular weight protamine (LMWP) 与 EGF (2 μM; 0.5-24 h) 偶联后，对三维人工人体皮肤模型的渗透性显著增强；在 2 μM 的加载浓度下，24 h 后检测到的累积渗透浓度为 0.129 μM^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Low molecular weight protamine (LMWP)-gelonin conjugate (110 μg；瘤周注射；15 天内给药 9 次) 可显著诱导结肠腺癌肿瘤消退，将 BALB/c 小鼠的平均肿瘤重量降至 0.33 g^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1880.18 (free base)

C₇₂H₁₄₂N₄₄O₁₆·xC₂H₄O₂

固体

Val-Ser-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Gly-Arg-Arg-Arg-Arg

VSRRRRRRGGRRRR

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Chang LC, et al. Low molecular weight protamine (LMWP) as nontoxic heparin/low molecular weight heparin antidote (II): in vitro evaluation of efficacy and toxicity. AAPS PharmSci. 2001;3(3):E18.  [Content Brief]

  [2]. Park YJ, et al. Nontoxic membrane translocation peptide from protamine, low molecular weight protamine (LMWP), for enhanced intracellular protein delivery: in vitro and in vivo study. FASEB J. 2005;19(11):1555-1557.  [Content Brief]

  [3]. Choi JK, et al. The effect of epidermal growth factor (EGF) conjugated with low-molecular-weight protamine (LMWP) on wound healing of the skin. Biomaterials. 2012;33(33):8579-8590.  [Content Brief]