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Art. -Nr.: HY-150972

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P163-0892

P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration.

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CAS. Nr.: 1574576-45-6
Formel: C₁₉H₂₀N₂O₃S
Molecular Weight:356.44

Speicherung:

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

Data Sheet (275 KB)

P163-0892 Chemical Structure

CAS. Nr.: 1574576-45-6

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	>256 μg/mL Compound: P163-0892; R-0892	Cytotoxicity against human Caco-2 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay Cytotoxicity against human Caco-2 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay	[PMID: 35922963]
Erythrocyte	IC₅₀	>256 μg/mL Compound: P163-0892; R-0892	Cytotoxicity against rabbit RBC assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay Cytotoxicity against rabbit RBC assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay	[PMID: 35922963]
HUVEC	IC₅₀	>64 μg/mL Compound: P163-0892; R-0892	Cytotoxicity against human HUVEC cells assessed as inhibition on cell growth incubated for 24 hrs by CCK-8 assay Cytotoxicity against human HUVEC cells assessed as inhibition on cell growth incubated for 24 hrs by CCK-8 assay	[PMID: 35922963]

In Vitro

P163-0892 (0-32 μg/mL; 48 h) shows antifungal activity with a MIC of 0.25 μg/mL and 0.5 μg/mL against Cryptococcus neoformans and Cryptococcus gattii, respectively^[1].
P163-0892 has good aqueous solubility^[1].
P163-0892 has no cytotoxicity and no obvious cardiotoxicity^[1].

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

In Vivo

P163-0892 (10 mg/kg; 5 days) significantly extends the survival of larvae infected with either C. neoformans or C. gattii^[1].

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

Animal Model:

Wax moth larva infected with C. neoformans H99 or C. gattii WM178^[1]
Dosage:

10 mg/kg
Administration:

5 days
Result:

Increased the survival rate of larvae.

Animal Model:

Male Sprague–Dawley rats weighing 200–250 g^[1]
Dosage:

2 mg/kg or 5 mg/kg
Administration:

Intravenous or oral administration (Pharmacokinetic Analysis)

Result:

Pharmacokinetic Parameters of P163-0892^a^[1]

route	dose (mg/kg)	T_1/2 (h)	T_max (h)	AUC_0-inf (h•ng/mL)	Cl (mL/h/kg)	MRT_0-t (h)	Vd_ss (L/kg)	BA (%)
iv	2 mg/kg	7.61		749	172	2.63	7.12
po	5 mg/kg	15.3	3.17	NR		3.83	NR	0.8

^aAbbreviations: iv, intravenous; po, per os; T_1/2, half-life elimination in hours; T_max, time of maximal concentration in hours; AUC, area under the curve; Cl, clearance; MRT, mean residence time; V_dss, volume of distribution at the steady state; BA, bioavailability; NR, not reportable; n = 3.

Chemical Information

CAS. Nr. 1574576-45-6
Molecular Weight 356.44
Formel C₁₉H₂₀N₂O₃S
SMILES

O=C(C1=C(O)C2=C(C=CS2)N(CC3=CC=CC=C3)C1=O)NCCCC
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 (275 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]. Li L, et al. Discovery of Novel 7-Hydroxy-5-oxo-4,5-dihydrothieno[3,2-b]pyridine-6-carboxamide Derivatives with Potent and Selective Antifungal Activity against Cryptococcus Species. J Med Chem. 2022 Aug 3. [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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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