1. Metabolic Enzyme/Protease
  2. Tryptophan Hydroxylase
  3. Telotristat

Telotristat (Synonyms: LP-778902)

製品番号: HY-13055B 純度: 98.91%
取扱説明書

Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.

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Telotristat 構造式

Telotristat 構造式

CAS 番号 : 1033805-28-5

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 303 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 132 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 252 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 372 在庫あり
Estimated Time of Arrival: December 31
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

Other Forms of Telotristat:

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製品説明

Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.

IC50 & Target

IC50: 0.028 μM (tryptophan hydroxylase)[1]

体外実験

Telotristat is the active moiety of telotristat etiprate. Telotristat etiprate is an ethyl ester prodrug which is hydrolyzed to telotristat. Telotristat etiprate is orally available serotonin synthesis inhibitor for the treatment of carcinoid syndrome[1].

体内実験

Telotristat etiprate is present in very low levels after oral administration. These low levels are due to rapid hydrolysis into the active moiety telotristat. The half-life ranges from approximately 4-12 h. There is no accumulation of telotristat with multiple dose administration over 2 weeks. Exposure to telotristat is approximately dose proportional[1].

臨床実験
分子量

546.93

分子式

C₂₅H₂₂ClF₃N₆O₃

CAS 番号

1033805-28-5

SMILES

N[[email protected]@H](CC1=CC=C(C2=NC(N)=NC(O[[email protected]](C3=CC=C(Cl)C=C3N4N=C(C)C=C4)C(F)(F)F)=C2)C=C1)C(O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 33.33 mg/mL (60.94 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[2]

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].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[2]

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].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

TelotristatLP-778902LP778902LP 778902Tryptophan HydroxylaseInhibitorinhibitorinhibit

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製品名:
Telotristat
製品番号:
HY-13055B
数量:
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