Monocrotaline (Crotaline)   中文名称: 野百合碱

野百合碱是一种天然存在的配体，具有很强的抗肿瘤作用和剂量依赖性细胞毒性。在 HepG2 细胞上测试时，野百合碱的 IC50 为 24.966 µg/mL，体外遗传毒性为 IC50 的 2 倍 [2]。

高血压大鼠模型可以通过使用野百合碱的动物建模来创建。在大鼠中，MCT 会导致肺血管综合征，其典型表现为肺心病、肺动脉高压 (PH) 和增殖性肺血管炎 [3]。野百合碱诱导的动物模型的优点是与临床前模型中人类肺动脉高压（PAH）的几个重要方面非常相似，例如血管重塑、平滑肌细胞增殖、内皮功能障碍、炎症细胞因子上调和右心室衰竭。 [4]。野百合碱的施用导致与外周出血（PH）发病机制相关的多个途径发生改变，例如刺激糖酵解、增殖标记物升高、肉碱稳态紊乱、炎症和纤维化生物标记物升高以及谷胱甘肽产生。减少[5]。给予单剂量野百合碱（60 mg/kg ip）的大鼠肺动脉压力显着升高，右心室肥厚和肺动脉结构重塑也增加。然后，给予黄芪甲苷 IV (ASIV)，剂量为 10 和 30 mg/kg/d，持续 21 天。通过增强肺动脉重塑和炎症，ASIV可以预防肺动脉高压[7]。野百合碱（60 mg/kg；腹腔注射；单剂量）3-4 周后诱导大鼠肺动脉高压 (PAH) 模型 [7]。在左肺切除大鼠模型中，野百合碱（60 mg/kg；腹腔注射；单剂量）表现出显着的抗肿瘤功效以及剂量依赖性细胞毒性[9]。使用 1 N HCl 溶解野百合碱，然后用无菌盐水稀释，并使用 1 N NaOH 将 pH 调至 7.4 [7]。

细胞活力测定[2]
细胞类型： HepG2 细胞
测试浓度： 25、50、100 和 200 µg/mL
孵育时间：48小时
实验结果：诱导凋亡率呈剂量依赖性。

[1]. Gomez-Arroyo JG, et al. The monocrotaline model of pulmonary hypertension in perspective. Am J Physiol Lung Cell Mol Physiol. 2012 Feb 15;302(4):L363-9.
[2]. Kusuma SS, et al. Antineoplastic activity of monocrotaline against hepatocellular carcinoma. Anticancer Agents Med Chem. 2014;14(9):1237-48.
[3]. Wilson DW, et, al. Mechanisms and pathology of monocrotaline pulmonary toxicity. Crit Rev Toxicol. 1992;22(5-6):307-25.
[4]. Nogueira-Ferreira R, et al. Exploring the monocrotaline animal model for the study of pulmonary arterial hypertension: A network approach. Pulm Pharmacol Ther. 2015 Dec;35:8-16.
[5]. Rafikova O,et al. Metabolic Changes Precede the Development of Pulmonary Hypertension in the Monocrotaline Exposed RatLung. PLoS One. 2016 Mar 3;11(3):e0150480.
[6]. Wu XH, et al. Experimental animal models of pulmonary hypertension: Development and challenges. Animal Model Exp Med. 2022 Sep; 5(3):207-216.
[7]. Jin H, et al. Astragaloside IV blocks monocrotaline‑induced pulmonary arterial hypertension by improving inflammation and pulmonary artery remodeling. Int J Mol Med. 2021 Feb;47(2):595-606.
[8]. Chen JY, et al. An in vitro study on interaction of anisodine and monocrotaline with organic cation transporters of the SLC22 and SLC47 families. Chin J Nat Med. 2019 Jul;17(7):490-497.
[9]. Zhao J, et al. Effects of paclitaxel intervention on pulmonary vascular remodeling in rats with pulmonary hypertension. Exp Ther Med. 2019 Feb;17(2):1163-1170.

C16H23NO6

325.36

315-22-0

O=C(O[C@]1([H])CCN2[C@]1([H])C(CO3)=CC2)[C@H](C)[C@@](C)(O)[C@@](C)(O)C3=O

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

1M HCl : 200 mg/mL (~614.70 mM)
DMSO : ~25 mg/mL (~76.84 mM)
H2O : ~2 mg/mL (~6.15 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.68 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (7.68 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution.
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.

---

View More

Solubility in Formulation 3: ≥ 2.08 mg/mL (6.39 mM) 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 20.8 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 4: ≥ 2.08 mg/mL (6.39 mM) 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 20.8 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 5: ≥ 2.08 mg/mL (6.39 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

---

Solubility in Formulation 6: ≥ 0.5 mg/mL (1.54 mM)(saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.

---

Solubility in Formulation 7: 4.17 mg/mL (12.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C).

---

Solubility in Formulation 8: 21 mg/mL (64.54 mM) in 20% HP-β-CD in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; Need ultrasonic and warming and heat to 53°C.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。