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apremilast in vitro  (BPS Bioscience)


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    BPS Bioscience apremilast in vitro
    KVA-D-88 was administered into mice (n = 4) by either i.p. injection (10 mg/kg) or p.o. approach (10 mg/kg) and 30 min or 24 hours later, mice were sacrificed for the removal blood and brain. The concentrations of KVA-D-88 were determined in these two tissues to calculate the concentration ratio of brain vs. plasma. (A) Brain and plasma KVA-D-88 concentration 30 min after i.p. injection (n = 4). (B) The IC50 of KVA-D-88 on PDE4B and PDE4D in vitro. HEK293 cells were cultured and transfected with PDE4B1 expression vector, CRE luciferase reporter and a control renilla luciferase vector. The cells were dosed with KVA-D-88 and incubated overnight. Forskolin was added and incubated for 5 – 6 h. A dual luciferase assay was performed for measuring firefly luminescence. The intensity of renilla luminescence was served as internal control. Cell based assays were performed in triplicate at each concentration. The EC50 value was determined by the concentration causing a half-maximal percent activity. (C) The non-linear dose-response curve of KVA-D-88 on PDE4. (D) The non-linear dose-response curve of <t>apremilast</t> on PDE4. (E) The table of EC50 of KVA-D-88 and apremilast on PDE4 in vitro.
    Apremilast In Vitro, supplied by BPS Bioscience, used in various techniques. Bioz Stars score: 90/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/apremilast+in+vitro/Apremilast/pmc08383802-56-22-28
    Average 90 stars, based on 3 article reviews
    apremilast in vitro - by Bioz Stars, 2026-10
    90/100 stars

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    1) Product Images from "KVA-D-88, a novel preferable phosphodiesterase 4B inhibitor, decreases cocaine-mediated reward properties in vivo"

    Article Title: KVA-D-88, a novel preferable phosphodiesterase 4B inhibitor, decreases cocaine-mediated reward properties in vivo

    Journal: ACS chemical neuroscience

    doi: 10.1021/acschemneuro.0c00170

    KVA-D-88 was administered into mice (n = 4) by either i.p. injection (10 mg/kg) or p.o. approach (10 mg/kg) and 30 min or 24 hours later, mice were sacrificed for the removal blood and brain. The concentrations of KVA-D-88 were determined in these two tissues to calculate the concentration ratio of brain vs. plasma. (A) Brain and plasma KVA-D-88 concentration 30 min after i.p. injection (n = 4). (B) The IC50 of KVA-D-88 on PDE4B and PDE4D in vitro. HEK293 cells were cultured and transfected with PDE4B1 expression vector, CRE luciferase reporter and a control renilla luciferase vector. The cells were dosed with KVA-D-88 and incubated overnight. Forskolin was added and incubated for 5 – 6 h. A dual luciferase assay was performed for measuring firefly luminescence. The intensity of renilla luminescence was served as internal control. Cell based assays were performed in triplicate at each concentration. The EC50 value was determined by the concentration causing a half-maximal percent activity. (C) The non-linear dose-response curve of KVA-D-88 on PDE4. (D) The non-linear dose-response curve of apremilast on PDE4. (E) The table of EC50 of KVA-D-88 and apremilast on PDE4 in vitro.
    Figure Legend Snippet: KVA-D-88 was administered into mice (n = 4) by either i.p. injection (10 mg/kg) or p.o. approach (10 mg/kg) and 30 min or 24 hours later, mice were sacrificed for the removal blood and brain. The concentrations of KVA-D-88 were determined in these two tissues to calculate the concentration ratio of brain vs. plasma. (A) Brain and plasma KVA-D-88 concentration 30 min after i.p. injection (n = 4). (B) The IC50 of KVA-D-88 on PDE4B and PDE4D in vitro. HEK293 cells were cultured and transfected with PDE4B1 expression vector, CRE luciferase reporter and a control renilla luciferase vector. The cells were dosed with KVA-D-88 and incubated overnight. Forskolin was added and incubated for 5 – 6 h. A dual luciferase assay was performed for measuring firefly luminescence. The intensity of renilla luminescence was served as internal control. Cell based assays were performed in triplicate at each concentration. The EC50 value was determined by the concentration causing a half-maximal percent activity. (C) The non-linear dose-response curve of KVA-D-88 on PDE4. (D) The non-linear dose-response curve of apremilast on PDE4. (E) The table of EC50 of KVA-D-88 and apremilast on PDE4 in vitro.

    Techniques Used: Injection, Concentration Assay, In Vitro, Cell Culture, Transfection, Expressing, Plasmid Preparation, Luciferase, Incubation, Activity Assay

    Related Articles

    In Vitro:

    Article Title: KVA-D-88, a novel preferable phosphodiesterase 4B inhibitor, decreases cocaine-mediated reward properties in vivo
    Article Snippet: .. The EC 50 of KVA-D-88 to elevate cAMP levels was 0.5 μM, which is 10-fold lower, compared to the EC 50 of apremilast in vitro (data collected at BPS Biosciences, San Diego, CA). ..



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    KVA-D-88 was administered into mice (n = 4) by either i.p. injection (10 mg/kg) or p.o. approach (10 mg/kg) and 30 min or 24 hours later, mice were sacrificed for the removal blood and brain. The concentrations of KVA-D-88 were determined in these two tissues to calculate the concentration ratio of brain vs. plasma. (A) Brain and plasma KVA-D-88 concentration 30 min after i.p. injection (n = 4). (B) The IC50 of KVA-D-88 on PDE4B and PDE4D in vitro. HEK293 cells were cultured and transfected with PDE4B1 expression vector, CRE luciferase reporter and a control renilla luciferase vector. The cells were dosed with KVA-D-88 and incubated overnight. Forskolin was added and incubated for 5 – 6 h. A dual luciferase assay was performed for measuring firefly luminescence. The intensity of renilla luminescence was served as internal control. Cell based assays were performed in triplicate at each concentration. The EC50 value was determined by the concentration causing a half-maximal percent activity. (C) The non-linear dose-response curve of KVA-D-88 on PDE4. (D) The non-linear dose-response curve of <t>apremilast</t> on PDE4. (E) The table of EC50 of KVA-D-88 and apremilast on PDE4 in vitro.
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    KVA-D-88 was administered into mice (n = 4) by either i.p. injection (10 mg/kg) or p.o. approach (10 mg/kg) and 30 min or 24 hours later, mice were sacrificed for the removal blood and brain. The concentrations of KVA-D-88 were determined in these two tissues to calculate the concentration ratio of brain vs. plasma. (A) Brain and plasma KVA-D-88 concentration 30 min after i.p. injection (n = 4). (B) The IC50 of KVA-D-88 on PDE4B and PDE4D in vitro. HEK293 cells were cultured and transfected with PDE4B1 expression vector, CRE luciferase reporter and a control renilla luciferase vector. The cells were dosed with KVA-D-88 and incubated overnight. Forskolin was added and incubated for 5 – 6 h. A dual luciferase assay was performed for measuring firefly luminescence. The intensity of renilla luminescence was served as internal control. Cell based assays were performed in triplicate at each concentration. The EC50 value was determined by the concentration causing a half-maximal percent activity. (C) The non-linear dose-response curve of KVA-D-88 on PDE4. (D) The non-linear dose-response curve of apremilast on PDE4. (E) The table of EC50 of KVA-D-88 and apremilast on PDE4 in vitro.

    Journal: ACS chemical neuroscience

    Article Title: KVA-D-88, a novel preferable phosphodiesterase 4B inhibitor, decreases cocaine-mediated reward properties in vivo

    doi: 10.1021/acschemneuro.0c00170

    Figure Lengend Snippet: KVA-D-88 was administered into mice (n = 4) by either i.p. injection (10 mg/kg) or p.o. approach (10 mg/kg) and 30 min or 24 hours later, mice were sacrificed for the removal blood and brain. The concentrations of KVA-D-88 were determined in these two tissues to calculate the concentration ratio of brain vs. plasma. (A) Brain and plasma KVA-D-88 concentration 30 min after i.p. injection (n = 4). (B) The IC50 of KVA-D-88 on PDE4B and PDE4D in vitro. HEK293 cells were cultured and transfected with PDE4B1 expression vector, CRE luciferase reporter and a control renilla luciferase vector. The cells were dosed with KVA-D-88 and incubated overnight. Forskolin was added and incubated for 5 – 6 h. A dual luciferase assay was performed for measuring firefly luminescence. The intensity of renilla luminescence was served as internal control. Cell based assays were performed in triplicate at each concentration. The EC50 value was determined by the concentration causing a half-maximal percent activity. (C) The non-linear dose-response curve of KVA-D-88 on PDE4. (D) The non-linear dose-response curve of apremilast on PDE4. (E) The table of EC50 of KVA-D-88 and apremilast on PDE4 in vitro.

    Article Snippet: The EC 50 of KVA-D-88 to elevate cAMP levels was 0.5 μM, which is 10-fold lower, compared to the EC 50 of apremilast in vitro (data collected at BPS Biosciences, San Diego, CA).

    Techniques: Injection, Concentration Assay, In Vitro, Cell Culture, Transfection, Expressing, Plasmid Preparation, Luciferase, Incubation, Activity Assay