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TP0463518

カタログ番号GC31498

TP0463518 は、ヒト PHD2 に対して 5.3 nM の Ki 値を持つ強力な低酸素誘導因子プロリルヒドロキシラーゼ (PHD) 阻害剤です。

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TP0463518 化学構造

Cas No.: 1558021-37-6

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$178.00
在庫あり
5mg
$162.00
在庫あり
10mg
$252.00
在庫あり
25mg
$450.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of TP0463518

TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC50s of 18 and 63 nM as well as monkey PHD2 with an IC50 value of 22 nM[1].

Reference:
[1]. Kato S, et al. TP0463518, a novel inhibitor for hypoxia-inducible factor prolyl hydroxylases, increases erythropoietin in rodents and monkeys with a good pharmacokinetics-pharmacodynamics correlation. Eur J Pharmacol. 2018 Nov 5;838:138-144.

Chemical Properties of TP0463518

Cas No. 1558021-37-6 SDF
Canonical SMILES ClC(C=C1)=CC=C1OC2=NC=C(CN3C(C(C(NCC(O)=O)=O)=C(O)CC3)=O)C=C2
Formula C20H18ClN3O6 M.Wt 431.83
溶解度 DMSO : ≥ 125 mg/mL (289.47 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of TP0463518

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1 mg 5 mg 10 mg
1 mM 2.3157 mL 11.5786 mL 23.1573 mL
5 mM 0.4631 mL 2.3157 mL 4.6315 mL
10 mM 0.2316 mL 1.1579 mL 2.3157 mL
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In vivo Formulation Calculator (Clear solution) of TP0463518

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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