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United States

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製品番号: HY-155103

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Antitrypanosomal agent 15

Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an _pIC₅₀ of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2961381-94-0
分子式: C₂₁H₁₉FN₄O₄
分子量:410.40

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

Antitrypanosomal agent 15 構造式

CAS 番号: 2961381-94-0

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

Parasite アイソフォーム固有の製品をすべて表示 :

体外実験

Antitrypanosomal agent 15 (compound 26) has _pEC₅₀ of 6.1 and 4.4 against intracellular T. cruzi amastigotes and host VERO cells, and has efflux ratio of 1.8 and FaSSIF (the fasted state simulated intestinal fluid solubility) of 339 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Antitrypanosomal agent 15 (compound 26) (50 mg/kg b.i.d for 20 days, p.o.) shows good solubility and permeability, but has no curative towards in chronic mouse model of Chagas disease^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

The chronic mouse model of Chagas disease^[1]
Dosage:

50 mg/kg b.i.d for 20days
Administration:

Oral gavage (p.o.)
Result:

Was not curative .
Was above EC₉₉ for approximately 5 h after the first dose on day 1, but dropped to less than 2 h after the first dose by day 20.

化学情報

CAS 番号 2961381-94-0
分子量 410.40
分子式 C₂₁H₁₉FN₄O₄
SMILES

CNC(C1=C(F)C=CC(NC(C2=NN(C(C=C2)=O)CC3=CC=C(OC)C=C3)=O)=C1)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (280 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Thomas MG, et al. Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors. J Med Chem. 2023;66(15):10413-10431. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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分子量分子量

希釈計算機

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体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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