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Referencia número: 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.

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No. CAS: 1628945-93-6
Fòrmula: C₂₀H₂₀F₃N₃O₂
Peso molecular:391.39

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

BPN-14136 Chemical Structure

No. CAS: 1628945-93-6

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Descripciòn

Ver todos los productos específicos de isoformas Lipocalin Family :

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]

In Vitro

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 %	/	/	/

In Vivo

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.

Chemical Information

No. CAS 1628945-93-6
Peso molecular 391.39
Fòrmula 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
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Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

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Instrucciones de manejo (2659 KB)

Referencias

[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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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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BPN-14136

Ver todos los productos específicos de isoformas Lipocalin Family

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Referencias

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BPN-14136 Related Classifications

HY-182385 Related Classifications