2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. HIF-PHD-IN-1

HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia.

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

HIF-PHD-IN-1 Chemical Structure

HIF-PHD-IN-1 Chemical Structure

CAS No. : 1567657-46-8

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Based on 1 publication(s) in Google Scholar

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Description

HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia[1].

IC50 & Target

IC50: 54 nM (hHIF-PHD2)[1]
In Vivo

HIF-PHD-IN-1 (compound 19) (0.5-2 mg/kg; p. o. once daily for 4 weeks) improves hemoglobin levels in anemic rats[1].
HIF-PHD-IN-1 (10 mg/kg; single p.o.) increases serum erythropoietin (EPO) concentration at 8 h after administration in SD rats[1].
HIF-PHD-IN-1 (1 mg/kg; p.o.) shows good bioavailability (F=77%) in male SD rats[1].

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

Animal Model: Male SD Rats excising five-sixths of their kidneys[1]
Dosage: 0.5, 1, 2 mg/kg
Administration: P.o. once daily for 4 weeks
Result: Improved blood hemoglobin levels starting at weeks 2 and 1 in the groups receiving 1 and 2 (mg/kg)/day, respectively.
Animal Model: Male SD Rats[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: Single p.o. or i.v.
Result: Cmax=1839 ng/mL (p.o.); Cmax=12357ng/mL (i.v.); F=77%.
Molecular Weight

419.22

Formula

C17H12Cl2N6O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CN(C2=NC3=C(N([C@H](C4=CC(Cl)=CC=C4Cl)C)N=C3)C(N2)=O)N=C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (238.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3854 mL 11.9269 mL 23.8538 mL 59.6346 mL
5 mM 0.4771 mL 2.3854 mL 4.7708 mL 11.9269 mL
10 mM 0.2385 mL 1.1927 mL 2.3854 mL 5.9635 mL
15 mM 0.1590 mL 0.7951 mL 1.5903 mL 3.9756 mL
20 mM 0.1193 mL 0.5963 mL 1.1927 mL 2.9817 mL
25 mM 0.0954 mL 0.4771 mL 0.9542 mL 2.3854 mL
30 mM 0.0795 mL 0.3976 mL 0.7951 mL 1.9878 mL
40 mM 0.0596 mL 0.2982 mL 0.5963 mL 1.4909 mL
50 mM 0.0477 mL 0.2385 mL 0.4771 mL 1.1927 mL
60 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9939 mL
80 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7454 mL
100 mM 0.0239 mL 0.1193 mL 0.2385 mL 0.5963 mL
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HIF-PHD-IN-1 Related Classifications

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:

HIF-PHD-IN-11567657-46-8HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHhypoxia-induciblefactorprolylhydroxylasedomainHIF-PHD,renalanemiaInhibitorinhibitorinhibit

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