Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg |
ln Vivo |
HIF-PHD-IN-1 (compound 19) (0.5-2 mg/kg; orally, once day for 4 weeks) increases hemoglobin levels in anemic rats [1]. HIF-PHD-IN-1 (10 mg/kg; single oral dose) increases serum erythropoietin (EPO) concentration in SD rats 8 hours after delivery [1]. HIF-PHD-IN-1 (1 mg/kg; oral) showed high absorption (F=77%) in male SD rats [1].
|
---|---|
Animal Protocol |
Animal/Disease Models: Male SD rat, five-sixths of the kidneys were removed [1]
Doses: 0.5, 1, 2 mg/kg Route of Administration: Oral one time/day for 4 weeks Experimental Results: The treated group started from the 2nd week and Hemoglobin levels improved by 1 and 2 (mg/kg)/day starting in week 1, respectively. Animal/Disease Models: Male SD rat[1] Doses: 1 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Single oral or intravenous (iv) (iv)injection Experimental Results: Cmax=1839 ng/mL (oral); Cmax=12357ng/mL (iv); F=77%. |
References |
[1]. Goi T, et, al. Pyrazolo[4,3- d]pyrimidine Derivatives as a Novel Hypoxia-Inducible Factor Prolyl Hydroxylase Domain Inhibitor for the Treatment of Anemia. ACS Med Chem Lett. 2020 Jun 4; 11(7): 1416-1420.
|
Molecular Formula |
C17H12CL2N6O3
|
---|---|
Molecular Weight |
419.22
|
CAS # |
1567657-46-8
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
N1(C2NC(=O)C3N([C@H](C4=CC(Cl)=CC=C4Cl)C)N=CC=3N=2)C=C(C(O)=O)C=N1
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~100 mg/mL (~238.54 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3854 mL | 11.9269 mL | 23.8538 mL | |
5 mM | 0.4771 mL | 2.3854 mL | 4.7708 mL | |
10 mM | 0.2385 mL | 1.1927 mL | 2.3854 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.