Telotristat
(Synonyms: LP778902) 目录号 : GC16279A TPH1 inhibitor
Cas No.:1033805-28-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
BON CBA cells are grown in equal volume of DMEM and F12K with 5% bovine serum for 3-4 hours (20 K cell/well) and telotristat is added at a concentration range of 0.07 to 50 μM. The cells are incubated at 37°C overnight. 50 μM of the culture supernatant is then taken for 5HTP measurement. The supernatant is mixed with equal volume of 1M TCA, then filtered through glass fiber. The filtrate is loaded on reverse phase HPLC for 5HTP concentration measurement. The cell viability is measured by treating the remaining cells with Celltiter-Glo Luminescent Cell Viability Assay[2]. |
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Animal experiment: |
Rats: 14-week-old male C57 albino mice are dosed once daily by oral gavage at 5-10 mL/kg for four consecutive days. Five hours after the last dose, the animals are quickly sacrificed. 5-HT is extracted from the blood or tissues and measured by HPLC. Blood samples are taken for exposure analysis[2]. |
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References: [1]. Lapuerta P, et al. Telotristat etiprate, a novel inhibitor of serotonin synthesis for the treatment of carcinoid syndrome. Clin. Invest. (Lond.) (2015) 5(5), 447–456 |
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Telotristat is a tryptophan hydroxylase 1 (TPH1) inhibitor (IC50 = 16 nM).[1] Dietary administration of telotristat to pregnant and lactating mice decreases serotonin levels in maternal serum and decreases the femoral bone volume to tissue volume ratio, trabecular number and thickness, and cortical tissue mineral density, as well as serum calcium levels, in pups.[2]
Reference:
[1]. Goldberg, D.R., De Lombaert, S., Aiello, R., et al. Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors. Bioorg. Med. Chem. Lett. 26(12), 2855-2860 (2016).
[2]. Weaver, S.R., Fricke, H.P., Xie, C., et al. Peripartum dietary supplementation of a small-molecule inhibitor of tryptophan hydroxylase 1 compromises infant, but not maternal, bone. Am. J. Physiol. Endocrinol. Metab. 215(6), E1133-E1142 (2018).
| Cas No. | 1033805-28-5 | SDF | |
| 别名 | LP778902 | ||
| 化学名 | (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid | ||
| Canonical SMILES | CC1=NN(C=C1)C2=C(C=CC(=C2)Cl)C(C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)CC(C(=O)O)N)N | ||
| 分子式 | C25H22ClF3N6O3 | 分子量 | 546.93 |
| 溶解度 | 0.5mg/mL in ethanol, 10mg/mL in DMSO, or DMF | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8284 mL | 9.1419 mL | 18.2839 mL |
| 5 mM | 0.3657 mL | 1.8284 mL | 3.6568 mL |
| 10 mM | 0.1828 mL | 0.9142 mL | 1.8284 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。