2. Metabolic Enzyme/Protease
  3. Lipocalin Family
  4. 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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BPN-14136

BPN-14136 Chemical Structure

CAS No. : 1628945-93-6

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BPN-14136 Related Antibodies

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Retinol Binding Protein

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Description

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[1].

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.

BPN-14136 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUClast AUCINF_obs Bioavailability C0 CL Vss
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.
Molecular Weight

391.39

Formula

C20H20F3N3O2
CAS No.
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.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BPN-14136 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BPN-141361628945-93-6BPN14136BPN 14136Lipocalin Familytransthyretinretinal pigment epitheliumrat liver microsomeCYPhERGRetinol Binding Protein 4RBP4Stargardt diseasehuman liver microsomeatrophic age-related macular degenerationInhibitorinhibitorinhibit

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