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Cat. No.: HY-108044

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ONO-5334

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with K_i values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC₅₀ value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.

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

CAS No.: 868273-90-9
Formula: C₂₁H₃₄N₄O₄S
Molecular Weight:438.58

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ONO-5334 Chemical Structure

CAS No.: 868273-90-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

cathepsin K

All Cathepsin Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Vero C1008	EC₅₀	0.5 μM Compound: ONO 5334	Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs	[PMID: 32511357]
Vero C1008	EC₅₀	0.5 μM Compound: ONO 5334	Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs	10.1101/2020.04.16.044016

In Vitro

ONO-5334 has inhibitory effects on human cathepsin S, human cathepsin L, human cathepsin B, porcine calpain Ι and porcine calpain II with K_i values of 0.83 nM, 1.7 nM, 32 nM, 82 nM and 69 nM, respectively^[1].
ONO-5334 (0.1-1 μM; 24 hours) suppresses human osteoclast-mediated bone resorption. It potently reduces osteoclast-mediated release of CTX from bone slices as a dose dependent manner^[1].
ONO-5334 (0-10 μM; pre-treated for 16 h) inhibits antiviral activities in a discernable dose-dependent manner in Vero E6 cells by designed to capture multicycle replication, exhibiting an EC₅₀ value of 0.5 μM^[2]/

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

Cell Viability Assay^[2]

Cell Line:

Vero E6 cells
Concentration:

0.001 μM, 0.003 μM, 0.1 μM, 0.3 μM, 1 μM, 2.5 μM
Incubation Time:

Pre-treated for 16 h and then cultured for 24 hours
Result:

Inhibited SARS-COV-2 virus replication in a dose-dependent manner.

In Vivo

ONO-5334 (oral administration; 0.12-15 mg/kg; single dose) can dose-dependently reduce PTHrP-induced increase in plasma calcium with significant effect (86% reduction) at 15 mg/kg. It also reduces PTHrP-induced increase in plasma CTX level in TPTX rats by 90% at 15 mg/kg^[1].
ONO-5334 (oral administration; 0.3-30 mg/kg; 7 consecutive days) at 3 mg/kg or 30 mg/kg significantly decreases CTX (a bone resorption marker) concentration. On day 7, the reduction in serum CTX concentration by ONO-5334 at 3 mg/kg and 30 mg/kg was 62% and 79%, respectively^[1].

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

Animal Model:

Monkey^[1]
Dosage:

0.3 mg/kg; 3 mg/kg
Administration:

Oral administration; 7 consecutive days
Result:

Reduced bone resorption markers but not bone formation markers in normal monkeys.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 868273-90-9
Appearance Solid
Molecular Weight 438.58
Formula C₂₁H₃₄N₄O₄S
Color Off-white to light yellow
SMILES

O=C(C(N/N=C(SC[C@H]1C)/N1C)=O)[C@H](C2CCOCC2)NC(C3CCCCCC3)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Nucleic Acids Res

COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]

2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390
Sci Rep

Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]

2022 Jul 16;12(1):12197. PMID: 35842458

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (114.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2801 mL

11.4004 mL

22.8009 mL

5 mM

0.4560 mL

2.2801 mL

4.5602 mL

10 mM

0.2280 mL

1.1400 mL

2.2801 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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)

References

[1]. Ochi Y, et al. Effects of ONO-5334, a novel orally-active inhibitor of cathepsin K, on bone metabolism. Bone. 2011 Dec;49(6):1351-6. [Content Brief]

[2]. Laura Riva, et al.A Large-scale Drug Repositioning Survey for SARS-CoV-2 Antivirals. bioRxiv. 2020 Apr 17;2020.04.16.044016. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.2801 mL	11.4004 mL	22.8009 mL	57.0021 mL
	5 mM	0.4560 mL	2.2801 mL	4.5602 mL	11.4004 mL
	10 mM	0.2280 mL	1.1400 mL	2.2801 mL	5.7002 mL
	15 mM	0.1520 mL	0.7600 mL	1.5201 mL	3.8001 mL
	20 mM	0.1140 mL	0.5700 mL	1.1400 mL	2.8501 mL
	25 mM	0.0912 mL	0.4560 mL	0.9120 mL	2.2801 mL
	30 mM	0.0760 mL	0.3800 mL	0.7600 mL	1.9001 mL
	40 mM	0.0570 mL	0.2850 mL	0.5700 mL	1.4251 mL
	50 mM	0.0456 mL	0.2280 mL	0.4560 mL	1.1400 mL
	60 mM	0.0380 mL	0.1900 mL	0.3800 mL	0.9500 mL
	80 mM	0.0285 mL	0.1425 mL	0.2850 mL	0.7125 mL
	100 mM	0.0228 mL	0.1140 mL	0.2280 mL	0.5700 mL

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
Purity & Documentation
References

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ONO-5334

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ONO-5334

All Cathepsin Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ONO-5334

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ONO-5334

All Cathepsin Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ONO-5334 Related Classifications

Cat. No.: HY-108044