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製品番号: HY-189007

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P2X2/3-antagonist-1

P2X2/3-antagonist-1 is a P2X2/3 purinergic receptor antagonist and taste blocker. P2X2/3-antagonist-1 binds to an allosteric site, induces a concentration-dependent rightward shift of the concentration-response curve of the α,β-Me-ATP agonist, and shares the binding site with AF-353 (HY-14483). P2X2/3-antagonist-1 blocks bitter taste perception in mice and abolishes their preference for plain water over bitter Quinine (HY-D0143) solution.

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。

分子式: C₁₈H₂₀IN₅O₄
分子量:497.29

保管条件:

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

P2X2/3-antagonist-1 構造式

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
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

P2X2 Receptor

P2X3 Receptor

P2X Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

P2X2/3-antagonist-1 potently (compound 30) inhibits human P2X2/3 receptor activity in CHO cells coexpressing human P2X2 and P2X3 with a pIC₅₀ of 8.1^[1].
P2X2/3-antagonist-1 (1 nM-1 μM; 30 nM) acts as an allosteric antagonist of human P2X2/3 receptors in CHO cells coexpressing human P2X2 and P2X3, with a pK_B of 8.7, and shares a binding site with AF-353 (1)^[1].
P2X2/3-antagonist-1 exhibits moderate-high permeability in MDCK wild-type cells, with a P_app value of 6.2 × 10^-6 cm/s^[1].
P2X2/3-antagonist-1 has a kinetic solubility of 106 μM in PBS at pH 7.4^[1].
P2X2/3-antagonist-1 has a log D value of 3.2 in 1-octanol/PBS at pH 7.4^[1].
P2X2/3-antagonist-1 (10 μM) has a low risk of cytochrome P450-related interactions, with weak inhibition of CYP2C8 and CYP2C9 at 10 μM and no time-dependent inhibition of CYP3A4^[1].
P2X2/3-antagonist-1 (30 μM) exhibits minimal off-target activity in a 47-target safety panel, with only 54% inhibition of CCK1 at 30 μM^[1].

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

Parmacokinetics

Species	Dose	Route	CL_plasma	V_ss	T_1/2	Bioavailability
Mice^[1]	1 mg/kg	i.v.	130 mL/min/kg	2.7 L/kg	0.6 h	/
Mice^[1]	1 mM	p.o.	/	/	/	62 %

化学情報

分子量 497.29
分子式 C₁₈H₂₀IN₅O₄
SMILES

CC(C)C1=C(OC(C=N2)=C(N)N3C2=CC(C(NCCO)=O)=N3)C=C(I)C(O)=C1
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

取扱説明書 (2659 KB)

参考文献

[1]. Saint-Dizier F, et al. Discovery of a Novel P2X2/3 Allosteric Antagonist as an Efficient Bitter Taste Blocker. Journal of medicinal chemistry. 2026 Aug 13;69(15):18856-18868.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Bioz

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MOQ

Minimum order quantity

100 mg

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