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製品番号: HY-182385

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BPN-14136

BPN-14136 is an orally effective retinol-binding protein 4 (RBP4) inhibitor. BPN-14136 inhibits the binding of retinol to RBP4 with an IC₅₀ of 12.8 nM. BPN-14136 inhibits retinol-dependent RBP4-transthyretin interaction (IC₅₀ = 43.6 nM) and reduces circulating plasma RBP4 levels in vivo. BPN-14136 decreases the formation of cytotoxic bisretinoids in retinal pigment epithelial cells. BPN-14136 can be used for the research of atrophic age-related macular degeneration and Stargardt disease.

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: 1628945-93-6
分子式: C₂₀H₂₀F₃N₃O₂
分子量:391.39

保管条件:

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

BPN-14136 構造式

CAS 番号: 1628945-93-6

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Fluorescent Dye

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

生物活性
- 製品説明
- Cellular Effect
- 体外実験
- Parmacokinetics
- 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
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関連分類
Bioz

生物活性

製品説明

Lipocalin Family アイソフォーム固有の製品をすべて表示 :

Retinol Binding Protein

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	30 μM Compound: 33	Inhibition of human ERG expressed in HEK293 cells by patch clamp assay Inhibition of human ERG expressed in HEK293 cells by patch clamp assay	[PMID: 26181715]

体外実験

BPN-14136 (Compound 33) (10 μM; 30 min) shows excellent stability in human and rat liver microsome assays, with 94% and 93% remaining after 30 min of incubation at 10 μM, respectively^[1].
BPN-14136 has a favorable in vitro ADMET profile, including high solubility, very low hepatic clearance, no significant CYP or hERG inhibition, high plasma protein binding, and high MDR1-MDCK permeability^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_last	AUC_{INF_obs}	Bioavailability	C₀	CL	V_ss
Rat^[1]	5.1 μmol/Kg	i.v.	/	/	22.0 h	795 μM·h	1017 μM·h	/	58.6 μM	5.06 mL/min/kg	156 mL/kg
Rat^[1]	12.7 μmol/Kg	p.o.	62.2 μM	2.67 h	38.8 h	2011 μM·h	3636 μM·h	143 %	/	/	/

体内実験

BPN-14136 (Compound 33) (5 mg/kg; p.o.; single dose, daily; 7 days) induces robust plasma RBP4 lowering, with an 85% reduction after a single dose and a 95% reduction after 7 days of daily dosing^[1].

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

Animal Model:

Sprague-Dawley (male, adult, drug-naive)^[1]
Dosage:

5 mg/kg (single dose); 5 mg/kg (7-day daily dosing)
Administration:

p.o.; single dose; 7 days
Result:

Induced an 85% maximum decrease in plasma RBP4.
Induced an approximately 95% reduction in plasma RBP4.

化学情報

CAS 番号 1628945-93-6
分子量 391.39
分子式 C₂₀H₂₀F₃N₃O₂
SMILES

FC(F)(C1=C(C=CC=C1)[C@@H]2C[C@@]3([H])[C@@](CN(C4=NC(C)=CC(C(O)=O)=N4)C3)([H])C2)F
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]. Cioffi CL, et al. Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease. J Med Chem. 2015;58(15):5863-5888. [Content Brief]

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モル濃度計算機

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

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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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100 mg

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- 体内実験
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純度とドキュメンテーション
参考文献

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BPN-14136

Lipocalin Family アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

BPN-14136 関連分類

HY-182385 関連分類