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製品番号: HY-122561

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MK-1925

MK-1925 is an orally active, CNS-penetrant ORL1 receptor antagonist with an IC₅₀ of 8.2 nM. MK-1925 selectively inhibits the ORL1 receptor and shows no significant activity against other opioid receptors or the hERG potassium channel.

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: 932705-04-9
分子式: C₁₉H₂₁F₃N₄
分子量:362.40

保管条件:

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

Data Sheet (268 KB)

MK-1925 構造式

CAS 番号: 932705-04-9

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
- Cellular Effect
- 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
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生物活性

製品説明

Opioid Receptor アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>10 μM Compound: 39, MK-1925	Displacement of [3H]diprenorphin from human cloned mu opioid receptor expressed in CHO cells Displacement of [3H]diprenorphin from human cloned mu opioid receptor expressed in CHO cells	[PMID: 19564110]
CHO	IC₅₀	9800 nM Compound: 39, MK-1925	Displacement of [3H]U69593 from human cloned kappa opioid receptor expressed in CHO cells Displacement of [3H]U69593 from human cloned kappa opioid receptor expressed in CHO cells	[PMID: 19564110]
HEK293	IC₅₀	9500 nM Compound: 39, MK-1925	Displacement of [35S]MK499 from human ERG expressed in HEK293 cells overexpressing Ikr channel protein Displacement of [35S]MK499 from human ERG expressed in HEK293 cells overexpressing Ikr channel protein	[PMID: 19564110]

体外実験

MK-1925 (compound 39) is highly selective for ORL1 receptors over human μ, κ, and δ opioid receptors, with ORL1 binding IC₅₀ of 8.2 nM and minimal binding to other opioid receptors (IC₅₀ values ≥9800 nM or >10,000 nM)^[1].
MK-1925 has minimal binding affinity for hERG potassium channels, with an IC₅₀ of 9500 nM^[1].

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

Parmacokinetics

Species	Dose	Route	CL_plasma	V_dss	AUC_0-inf	C_max	T_1/2	Bioavailability
Rat^[1]	1 mg/kg	i.v.	83 mL/min/kg	5.2 L/kg	/	/	/	/
Rat^[1]	3 mg/kg	p.o.	/	/	0.3 μM·h	0.40 μM	0.7 h	21 %
Dog^[1]	1 mg/kg	i.v.	37 mL/min/kg	3.5 L/kg	/	/	/	/
Dog^[1]	3 mg/kg	p.o.	/	/	1.3 μM·h	2.6 μM	2.8 h	/

化学情報

CAS 番号 932705-04-9
分子量 362.40
分子式 C₁₉H₂₁F₃N₄
SMILES

C(CC#N)N1C(=C(C)C(CN[C@@H]2C[C@H](F)CC2)=N1)C3=CC(F)=CC(F)=C3
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 (268 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]. Kobayashi K, et al. Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist. Bioorg Med Chem Lett. 2009;19(16):4729-4732. [Content Brief]

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.

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Keywords

MOQ

Minimum order quantity

100 mg

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