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United States

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製品番号: HY-132303

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MK-8262

MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC₅₀ of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.

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: 1432054-03-9
分子式: C₃₅H₂₅F₉N₂O₅
分子量:724.57

保管条件:

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

Data Sheet (280 KB)

MK-8262 構造式

CAS 番号: 1432054-03-9

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
- IC₅₀ & Target
- 体外実験
- 体内実験
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

IC50: 53 nM (CETP)^[1]

体外実験

MK-8262 (Compound 87) reduces cell viability in a dose-dependent manner beginning at ∼10 μM in all 8 cell lines regardless of human CYP expression or glutathione depletion (HEK293/CYP cell lines expressing human CYP1A2, CYP2E1, CYP2D6, CYP2C8, CYP2B6, CYP3A4, CYP2C19, or CYP2C9)^[1].
MK-8262 has no effect on human CYP protein concentration or Nrf2 activation in any of the 8 cell lines^[1].

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

体内実験

MK-8262 (Compound 87; 10 mg/kg; orally) results in a significant HDL cholesterol increase in a 2-week chronic treatment of CETP transgenic mice^[1].
MK-8262 (1 mg/kg; iv) has a T_1/2 MRT of 6 hours, a CL of 2.6 mL/min•kg, and a V_ss of 0.95 L/kg for mouse^[1].
MK-8262 (2 mg/kg; po) has a C_max of 0.43 μM and an AUC of 7.9 μM•h for mouse^[1].
MK-8262 (1 mg/kg; iv) has a T_1/2 MRT of 13 hours, a CL of 3.1 mL/min•kg, and a V_ss of 2.4 L/kg for mouse^[1].
MK-8262 (2 mg/kg; po) has a C_max of 0.4 μM and an AUC of 9.7 μM•h for mouse^[1].

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

Related Protocols :

Research Protocol for Cardiovascular Diseases

化学情報

CAS 番号 1432054-03-9
分子量 724.57
分子式 C₃₅H₂₅F₉N₂O₅
SMILES

O=C(O)C1=CC=C(C2=CC(C3=CC=C(C(F)(F)F)C=C3[C@@H]4CC[C@]5([H])N4C(O[C@@H]5C6=CC(C(F)(F)F)=CC(C(F)(F)F)=C6)=O)=C(OC)N=C2)C(C)=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

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]. Petr Vachal, et al. Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties. J Med Chem. 2021 Aug 10. [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.

Bioz

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MOQ

Minimum order quantity

100 mg

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