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  2. Metabolic Enzyme/Protease Anti-infection
  3. Cathepsin SARS-CoV
  4. ONO-5334

ONO-5334 是一種強(qiáng)效、選擇性和口服活性的組織蛋白酶 K (cathepsin K) 抑制劑，對(duì)人、兔和大鼠組織蛋白酶 K 的作用值分別為 0.10 nM、0.049 nM 和 0.85 nM。ONO-5334 是一種有效的抗 SAR-COV-2 病毒活性的抗病毒化合物，其 EC50 值為 500 nM。ONO-5334 有潛力用于骨質(zhì)疏松癥以及 COVID-19 的相關(guān)研究。

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ONO-5334 Chemical Structure

ONO-5334 Chemical Structure

CAS No. : 868273-90-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥4824
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1 mg ￥2000
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5 mg ￥5000
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25 mg 現(xiàn)貨 詢價(jià)
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki 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[1].

IC50 & Target

cathepsin K

 

細(xì)胞效力
(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]
體外研究
(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 Ki 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]/

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.
體內(nèi)研究
(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].

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
分子量

438.58

Formula

C21H34N4O4S
CAS 號(hào)
性狀

固體

顏色

Off-white to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 50 mg/mL (114.00 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.2801 mL 11.4004 mL 22.8009 mL
5 mM 0.4560 mL 2.2801 mL 4.5602 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.83%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 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
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.

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產(chǎn)品名稱：
ONO-5334
目錄號(hào)：
HY-108044
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