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1mg |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
Vadadustat (formerly AKB-6548; PG-1016548; B-506; AKB6548; PG1016548; Vafseo) is a novel, potent, titratable and orally bioavailable hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with the potential for the treatment of anemia. It induces endogenous erythropoietin synthesis and enhances iron mobilization. As of 2020, it was approved by PMDA for the treatment of anemia caused by chronic kidney disease. Current treatment of anemia in chronic kidney disease (CKD) with erythropoiesis-stimulating agents can lead to substantial hemoglobin oscillations above target range and high levels of circulating erythropoietin.
ln Vitro |
Vadadustat improves iron mobilization and stimulates the body's natural production of erythropoietin. Vadadustat raises reticulocytes, plasma EPO, and Hb levels in a dose-dependent manner and is well tolerated in both healthy volunteers and patients with chronic renal disease. The vadadustat-induced increases in plasma EPO levels followed a typical diurnal pattern, peaking before the subsequent dose and being similar in size to physiological increases at moderate elevations. By raising transferrin levels and decreasing hepcidin, vadadustat promotes iron homeostasis. When compared to conventional ESAs, once-daily oral vadadustat that has been titrated to raise and maintain Hb within the target range may offer a number of benefits [1]. It has been noted that Vadadustat has a half-life of roughly 4.5 hours. The mean hemoglobin levels of the patients rose from 9.91 g/dL at baseline to 10.54 g/dL on day 29. From 334.1 ng/mL at baseline to 271.7 ng/mL on day 29, ferritin levels dropped [2].
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References |
[1]. Pergola PE, et al. Vadadustat, a novel oral HIF stabilizer, provides effective anemia treatment in nondialysis-dependent chronic kidney disease. Kidney Int. 2016 Nov;90(5):1115-1122.
[2]. Gupta N, et al. Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD. Am J Kidney Dis. 2017 Feb 24. pii: S0272-6386(17)30110-5. |
Molecular Formula |
C14H11CLN2O4
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Molecular Weight |
306.7011
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CAS # |
1000025-07-9
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SMILES |
O=C(O)CNC(C1=NC=C(C2=CC=CC(Cl)=C2)C=C1O)=O
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InChi Key |
JGRXMPYUTJLTKT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H11ClN2O4/c15-10-3-1-2-8(4-10)9-5-11(18)13(16-6-9)14(21)17-7-12(19)20/h1-6,18H,7H2,(H,17,21)(H,19,20)
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Chemical Name |
(5-(3-chlorophenyl)-3-hydroxypicolinoyl)glycine
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Synonyms |
AKB-6548; PG1016548; B-506; AKB 6548; PG 1016548; B506; AKB6548; PG-1016548;Vadadustat
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~326.05 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2605 mL | 16.3026 mL | 32.6052 mL | |
5 mM | 0.6521 mL | 3.2605 mL | 6.5210 mL | |
10 mM | 0.3261 mL | 1.6303 mL | 3.2605 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.