规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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靶点 |
hGHS-R1a ( Ki = 7 nM )
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体外研究 (In Vitro) |
Capromorelin 可刺激大鼠垂体细胞培养物中的 GH 释放,EC50 为 3 nM[2]。
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体内研究 (In Vivo) |
接受卡普莫瑞林 (30 mg/mL) 治疗的狗的食物消耗量明显高于接受安慰剂治疗的狗。卡普莫瑞林组的所有狗体重增加了 0.52 公斤,比安慰剂组多[1]。 Capromorelin 在啮齿类动物模型中表现出增强的肠道吸收,并表现出优异的药代动力学特性,包括在两种动物物种中的高生物利用度 [F(大鼠)= 65%,F(狗)= 44%][2]。 Capromorelin 可刺激麻醉大鼠模型中的 GH 释放,静脉注射 ED50 为 0.05 mg/kg [2]。
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酶活实验 |
将质粒pcDNA3.1neo中的人GHS-R1a受体cDNA转染至HEK293细胞(ATCC)中以产生膜。竞争性放射性配体结合测定使用已预先浸泡在 0.3% 聚乙烯亚胺中的 GF/C 过滤器以 96 孔形式进行。测试在室温下重复进行一小时,使用 50 pM [125I]-ghrelin 和每孔 1 μg 膜,溶于 50 mM HEPES、pH 7.4、10 mM MgCl2< /sub>、0.2% 牛血清白蛋白,以及随后的蛋白酶抑制剂:100 μg/mL 苯甲脒、100 μg/mL 杆菌肽、5 μg/mL 抑肽酶和 5 μg/mL 亮肽素。收获膜后,在 pH 7.4、50 mM HEPES 和 10 mM MgCl2 的冰冷缓冲液中冲洗 3 次。 GraphpadTM 的 Prism 用于计算 IC50 和 Ki 值。经测定,[125I]-ghrelin 在表达人 GHS 受体的膜上的 Kd 为 0.2 nM。
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动物实验 |
The study evaluated a flavored oral solution containing 30 mg/mL of capromorelin in comparison to a matched placebo-flavored oral solution treatment that was given for four days and contained all the formulation's ingredients but no capromorelin. Two groups of dogs are randomly assigned; Group 1 receives a placebo (0.1 mL/kg), while Group 2 receives 3.0 mg/kg. Each day, at around nine in the morning, both groups receive the same treatment. Day 0 is the first day of medication. A syringe inserted into the mouth's corner is used to administer both the test medication and the placebo. When calculating doses, the Day 0 weight is utilized.
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参考文献 |
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分子式 |
C32H41N5O10
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分子量 |
655.705
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精确质量 |
655.29
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元素分析 |
C, 58.62; H, 6.30; N, 10.68; O, 24.40
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CAS号 |
193273-69-7
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相关CAS号 |
193273-66-4; 193273-69-7 (tartrate)
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外观&性状 |
Solid powder
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SMILES |
CC(C)(C(=O)N[C@H](COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)[C@@]3(C2)CC4=CC=CC=C4)C)N.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
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InChi Key |
MJGRJCMGMFLOET-MYPSAZMDSA-N
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InChi Code |
InChI=1S/C28H35N5O4.C4H6O6/c1-27(2,29)25(35)30-22(18-37-17-21-12-8-5-9-13-21)24(34)33-15-14-23-28(19-33,26(36)32(3)31-23)16-20-10-6-4-7-11-20;5-1(3(7)8)2(6)4(9)10/h4-13,22H,14-19,29H2,1-3H3,(H,30,35);1-2,5-6H,(H,7,8)(H,9,10)/t22-,28-;1-,2-/m11/s1
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化学名 |
N-[(2R)-1-[(3aR)-3a-benzyl-2-methyl-3-oxo-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-1-oxo-3-phenylmethoxypropan-2-yl]-2-amino-2-methylpropanamide;(2R,3R)-2,3-dihydroxybutanedioic acid
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别名 |
Capromorelin tartrate; CP424,391; CP-424391; CP-424,391; CP 424,391;CP 424391; CP424391; CP-424,391-18
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO: ~100 mg/mL (~152.5 mM)
H2O: ~100 mg/mL (~152.5 mM) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.81 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 (3.81 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 (3.81 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: 50 mg/mL (76.25 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 | 1.5251 mL | 7.6253 mL | 15.2506 mL | |
5 mM | 0.3050 mL | 1.5251 mL | 3.0501 mL | |
10 mM | 0.1525 mL | 0.7625 mL | 1.5251 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) 。
Mean (±SD) food consumption in dogs (n = 6 males and 6 females/group) treated with placebo (◊) or capromorelin (●) oral solution. Day 0 is the first day of dosing. BMC Vet Res . 2017 Jan 5;13(1):10. td> |