2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. Vadadustat prodrug-1

Vadadustat prodrug-1 is a near-infrared activated photocaged, blood-brain barrier-permeable neuroprotective prodrug of Vadadustat. Vadadustat prodrug-1 masks the acidic pharmacophore of Vadadustat, and releases active Vadadustat upon irradiation at 650 nm to inhibit PHD2. Vadadustat prodrug-1 reduces cell damage, infarct volume and cerebral edema, and promotes neurological function recovery. Vadadustat prodrug-1 can be used for the research of ischemic stroke.

For research use only. We do not sell to patients.

Vadadustat prodrug-1

Vadadustat prodrug-1 Chemical Structure

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Vadadustat prodrug-1 Related Antibodies

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Description

Vadadustat prodrug-1 is a near-infrared activated photocaged, blood-brain barrier-permeable neuroprotective prodrug of Vadadustat. Vadadustat prodrug-1 masks the acidic pharmacophore of Vadadustat, and releases active Vadadustat upon irradiation at 650 nm to inhibit PHD2. Vadadustat prodrug-1 reduces cell damage, infarct volume and cerebral edema, and promotes neurological function recovery. Vadadustat prodrug-1 can be used for the research of ischemic stroke[1].

In Vitro

Vadadustat prodrug-1 (Compound 11) (100 μM; 1-10 min irradiation) enables complete and rapid near-infrared-induced photorelease of Vadadustat (HY-101277) within 10 min under physiological conditions, and exhibits excellent stability under white light, reductive environments and physiological temperatures[1].
Vadadustat prodrug-1 (10 min irradiation prior to 1 h incubation) potently inhibits PHD2 only after 10 min of irradiation at 650 nm, with an IC50 of 71.6 nM, and shows no activity under dark conditions[1].
Vadadustat prodrug-1 (5-10 μM; 24 h reoxygenation, 10 min irradiation where applicable) exerts dose-dependent neuroprotective effects on HT22 cells treated with oxygen-glucose deprivation/reoxygenation (OGD/R). It enhances cell viability, increases the number of viable cells and reduces the number of dead cells only after 10 min of 650 nm irradiation, with no effect under dark conditions[1].
Vadadustat prodrug-1 (5-10 μM; 10 min irradiation where applicable) dose-dependently stabilizes HIF-1α in HT22 cells, reduces OGD/R-induced ROS accumulation, restores SOD activity and mitochondrial membrane potential, and decreases MDA levels [1], but only after 10 min of irradiation with 650 nm light.

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

Vadadustat prodrug-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HT22 cells (oxygen-glucose deprivation/reoxygenation (OGD/R) treated)
Concentration: 5, 10 μM
Incubation Time: 24 h (reoxygenation; 10 min irradiation where applicable)
Result: Improved cell viability in a dose-dependent manner with 650 nm irradiation, with efficacy comparable to Vadadustat.
Showed no protective effect without irradiation, with cell viability matching the OGD/R control group.

Western Blot Analysis[1]

Cell Line: HT22 cells
Concentration: 5-10 μM
Incubation Time: 10 min (irradiation where applicable)
Result: Dose-dependently upregulated HIF-1α protein levels in HT22 cells after 10 min of 650 nm irradiation, with an effect comparable to equimolar concentrations of Vadadustat.
Parmacokinetics
Species Dose Route Plasma Concentration Brain Concentration
Mice[1] 2 mg/kg s.c. 254.78 ng/mL 44.77 ng/g
Mice[1] 2 mg/kg s.c. 267.32 ng/mL 389.70 ng/g
In Vivo

Vadadustat prodrug-1 (20-50 mg/kg; s.c.; 30 minutes pre-surgery, repeated at 24 and 48 hours post-surgery; each dose followed by 650 nm light irradiation for 10 min) provides light-activated neuroprotection in a mouse ischemic stroke model, with the 50 mg/kg dose reducing cerebral infarct area by 53% and delivering superior dose-dependent improvements in neurological function, brain edema, neuronal structure, and survival compared to the 20 mg/kg dose[1].

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

Animal Model: ICR mice[1]
Dosage: 20 mg/kg; 50 mg/kg
Administration: s.c.; 30 minutes pre-surgery, repeated at 24 and 48 hours post-surgery; each dose followed by 650 nm light irradiation for 10 min
Result: Reduced cerebral infarct area by 33% at 20 mg/kg, comparably to positive control edaravone.
Decreased brain water content at 20 mg/kg, outperforming edaravone.
Improved modified neurological severity score (mNSS) more effectively than edaravone at 20 mg/kg.
Reduced cerebral infarct area by 53% at 50 mg/kg.
Decreased brain water content at 50 mg/kg.
Provided superior dose-dependent improvement in mNSS at 50 mg/kg compared to 20 mg/kg dose and edaravone.
Upregulated HIF-1α levels in brain tissue in a dose-dependent manner at both doses.
Partially restored hippocampal architecture at both doses, with 50 mg/kg dose significantly increasing thickness and regularity of pyramidal layers in CA1 and CA3 regions.
Improved postoperative survival outcomes in a dose-dependent manner at both doses.
Molecular Weight

767.08

Formula

C44H40BClN4O6
SMILES

ClC1=CC(C2=CN=C(C(O)=C2)C(NCC(OCC(C3=CC4=C(N3[B-](C)5C)C(C=CC(OC)=C6)=C6CC4)=C7[N+]5=C8C9=C(CCC8=C7)C=C(OC)C=C9)=O)=O)=CC=C1
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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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Vadadustat prodrug-1 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:

Vadadustat prodrug-1Vadadustat prodrug1Vadadustat prodrug 1HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHSODmouse ischemic stroke modelMDAROSHIF-1αmitochondrial membrane potentialHT22 cellsischemic strokePHD2brain edemaInhibitorinhibitorinhibit

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