规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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50mg |
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100mg |
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500mg |
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Other Sizes |
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体内研究 (In Vivo) |
用 5 毫克/公斤/天的甲磺酸丁阿莫伦治疗的狗体重显着增加,并且血清中的 GH 和 IGF-1 水平更高。在研究第 7 天或第 15 天,甲磺酸咪唑啉导致脑脊液 IGF-1 或 GH 水平没有明显升高 [1]。甲磺酸布莫伦(50 μg,腹腔注射)在治疗前接受 GH 治疗的动物中不能激活这些神经元。 GH 和奥曲肽不会阻断甲磺酸伊布莫仑对基因敲除小鼠中的弓状神经元的刺激[2]。 GH 和 IGF-I 水平的显着增加与长期口服甲磺酸丁阿莫伦有关,并且这些作用在整个治疗过程中持续存在。给予甲磺酸伊布莫伦后,GH 谱较对照组表现出零星升高 [3]。口服治疗后,甲磺酸伊布莫伦可显着提高 GH 峰值浓度。口服或静脉注射时,甲磺酸伊布莫伦是一种强效 GH 促分泌素,可以快速、显着且持久地升高 GH 水平 [4]。
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参考文献 |
[1]. Prahalada S, et al. Insulin-like growth factor-1 and growth hormone (GH) levels in canine cerebrospinal fluid are unaffected by GH or GH secretagogue (MK-0677) administration. Horm Metab Res. 1999 Feb-Mar;31(2-3):133-7.
[2]. Zheng H, et al. Somatostatin receptor subtype 2 knockout mice are refractory to growth hormone-negative feedback on arcuate neurons. Mol Endocrinol. 1997 Oct;11(11):1709-17. [3]. Hickey GJ, et al. Repeat administration of the GH secretagogue MK-0677 increases and maintains elevated IGF-I levels in beagles. J Endocrinol. 1997 Feb;152(2):183-92. [4]. Jacks T, et al. MK-0677, a potent, novel, orally active growth hormone (GH) secretagogue: GH, insulin-like growth factor I, and other hormonal responses in beagles. Endocrinology. 1996 Dec;137(12):5284-9 |
分子式 |
C28H40N4O8S2
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分子量 |
624.77
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CAS号 |
159752-10-0
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SMILES |
S(C([H])([H])[H])(N1C2=C([H])C([H])=C([H])C([H])=C2C2(C1([H])[H])C([H])([H])C([H])([H])N(C([C@@]([H])(C([H])([H])OC([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])C(C(C([H])([H])[H])(C([H])([H])[H])N([H])[H])=O)=O)C([H])([H])C2([H])[H])(=O)=O.S(C([H])([H])[H])(=O)(=O)O[H]
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溶解度 (体外) |
H2O: ≥ 50 mg/mL (80.03 mM)
DMSO: 50 mg/mL (80.03 mM) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.00 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 (4.00 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (160.06 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. 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。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6006 mL | 8.0029 mL | 16.0059 mL | |
5 mM | 0.3201 mL | 1.6006 mL | 3.2012 mL | |
10 mM | 0.1601 mL | 0.8003 mL | 1.6006 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。