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Art. -Nr.: HY-155009

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PHD2-IN-1

PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC₅₀ of 22.53 nM. PHD2-IN-1 can be used for anemia research.

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CAS. Nr.: 2768219-28-7
Formel: C₂₁H₂₃ClN₄O₅
Molecular Weight:446.88

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

PHD2-IN-1 Chemical Structure

CAS. Nr.: 2768219-28-7

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC₅₀ of 22.53 nM. PHD2-IN-1 can be used for anemia research^[1].

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

In Vitro

PHD2-IN-1 (Compound 22) ( 0-50 μM; 12 hours) stabilizes HIF-α and increases the expression of the erythropoietin (EPO) gene^[1].

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

RT-PCR^[1]

Cell Line:

Hep3B cells
Concentration:

0,5,20,50 μM
Incubation Time:

12 hours
Result:

Significantly stabilized HIF-1α and HIF-2α.
Upregulated the EPO mRNA level in a dose-dependently manner.
Showed no significant effects on the expression of the VEGFA gene.

In Vivo

PHD2-IN-1 (Compound 22) (10,20,50 mg/kg, p.o., once daily for three days) stimulates erythropoiesis and increase reticulocytes in a dose-dependent manner in C57BL/6 mice^[1].
PHD2-IN-1 (50,100,200 mg/kg for i.p., once daily for 14 days) has no significant toxic reactions in ICR mice^[1].
PHD2-IN-1 (1 mg/kg for i.p., 10 mg/kg for p.o.) shows T_1/2s of 2.29 h (p.o.) or 3.72 h (i.v.) in rats and 1.17 h (p.o.) or 0.33 h (i.v.) in mice. And oral bioavailability (F%) of 33.9% in rats and 35.3% in mice^[1].
Pharmacokinetic parameters for PHD2-IN-1 (Compound 22) in SD rats and C57BL/6 mice ^[1]

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

Animal Model:

C57BL/6 mice^[1]
Dosage:

10,20, and 50 mg/kg
Administration:

Oral gavage (p.o.), once daily for three days
Result:

Increased reticulocytes in a dose-dependent manner.
The reticulocyte count/red blood cell count (RBC%) increased significantly in a dose-dependent manner.

Animal Model:

SD rats and C57BL/6 mice (Pharmacokinetic assay)^[1]
Dosage:

1, 10 mg/kg
Administration:

Intravenous injection (i.v.)，Oral gavage (p.o.)
Result:

Showed T_1/2s of 2.29 h (p.o.) or 3.72 h (i.v.) in rats and 1.17 h (p.o.) or 0.33 h (i.v.) in mice. And oral bioavailability (F%) of 33.9% in rats and 35.3% in mice.

Animal Model:

Subacute toxicity assessment in ICR mice^[1]
Dosage:

50,100,200 mg/kg
Administration:

Intraperitoneal injection (i.p.) once daily for 14 days
Result:

Had no significant hepatotoxicity or nephrotoxicity reactions after administration of a high dose of 200 mg/kg, at 10 imes the efficacious dose (20mg/kg).
Observed no death or behavioral abnormalities when the mice were treated in the dose of 800 mg/kg by p.o. administration.

Chemical Information

CAS. Nr. 2768219-28-7
Molecular Weight 446.88
Formel C₂₁H₂₃ClN₄O₅
SMILES

ClC1=CC=C(NCC(N2CCC(C3=CN=C(C(NCC(O)=O)=O)C(O)=C3)CC2)=O)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wu Y, et.al. Preferred Conformation-Guided Discovery of Potent and Orally Active HIF Prolyl Hydroxylase 2 Inhibitors for the Treatment of Anemia. J Med Chem. 2023 Jul 13;66(13):8545-8563. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Species	Route	Dose (mg/kg)	T_max (h)	C_max (ng/mL)	AUC_0-t (h•ng/mL)	AUC_0-Ꝏ (h•ng/mL)	T_1/2 (h)	CL (mL•min^-1/kg^-1)	V_Z (mL/kg)	MRT_0-Ꝏ (h)	F (%)
rat	p.o.	10	0.08	26140	7118	7135	2.29	1417	4629	0.56	33.9
rat	i.v.	1	/	/	2069	2106	3.72	483	2644	1.54	/
mice	p.o.	10	0.5	3036	4475	4489	1.17	2246	4532	1.67	35.3
mice	i.v.	1	/	/	1384	1387	0.33	721	345	0.53	/

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PHD2-IN-1

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PHD2-IN-1 Related Classifications

HY-155009 Related Classifications