T-1105,99.0%

产品编号:Bellancom-W015764| CAS NO:55321-99-8| 分子式:C5H5N3O2| 分子量:139.11

T-1105 是一种广谱病毒聚合酶 (polymerase) 抑制剂,T-705 的结构类似物,在转化为核糖核苷三磷酸 (RTP) 代谢物后抑制 RNA 病毒的聚合酶。T-1105 (Favipiravir) 对各种 RNA 病毒表现出抗病毒活性,包括寨卡病毒 (ZIKV),流感病毒,沙粒病毒,布尼亚病毒,西尼罗病毒 (WNV),黄热病病毒 (YFV) 和口蹄疫病毒 (FMDV)。T-1105 可由烟酰胺单核苷酸腺苷酰转移酶形成。

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Bellancom-W015764
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T-1105

产品介绍 T-1105,T-705 的结构类似物,是一种广谱 病毒聚合酶 (polymerase) 抑制剂。T-1105 在转化为核糖核苷三磷酸 (RTP) 代谢物后抑制 RNA 病毒的聚合酶。T-1105 对各种 RNA 病毒表现出抗病毒活性,T-1105 可由烟酰胺单核苷酸腺苷酰转移酶形成。
生物活性

T-1105, a structural analogue of T-705, is a novel broad-spectrum viral polymerase inhibitor. T-1105 inhibits the polymerases of RNA viruses after being converted to ribonucleoside triphosphate (RTP) metabolite. T-1105 has antiviral activity against various RNA viruses. T-1105 can be formed by nicotinamide mononucleotide adenylyltransferase.

体外研究

T-1105 has antiviral activity against various RNA viruses, including Zika virus (ZIKV), influenza virus, arenaviruses, bunyaviruses, West Nile virus (WNV), yellow fever virus (YFV), and foot-and-mouth disease virus (FMDV).
T-1105 has good anti-RNA virus activity with values EC50 of 17 μM and 24 μM for parainfluenza-3 virus and Punta Toro virus in MDCK cells.
T-1105 is a potential inhibitor of Zika virus replication[4].
T-1105 can inhibit the SFTSV replication with an value IC50 of 49 μM in Vero cells and is not affect cell viability in 0-3 μM[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[4]

Cell Line: Vero cells
Concentration: 1-4 μM
Incubation Time: 72 h
Result: Had potential antiviral activity against ZIKV strain SZ01 with an value EC50 of 97.5 μM in Vero cells.

Cell Viability Assay[5]

Cell Line: Vero cells
Concentration: 0-3 μM
Incubation Time: 4 h
Result: Did not affect cell viability in the test range (0-3 μM).
体内研究
(In Vivo)

T-1105 (Oral, 200 mg/kg, twice daily for 6 days) effectively inhibits the virus replication in the infected pigs[6].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pigs[6]
Dosage: 200 mg/kg
Administration: Oral, 200 mg/kg, twice daily for 6 days
Result: Reduced Viremia and increased anti-FMD antibody titers, did not observe any clinical signs of FMD.
体内研究

T-1105 (Oral, 200 mg/kg, twice daily for 6 days) effectively inhibits the virus replication in the infected pigs[6].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pigs[6]
Dosage: 200 mg/kg
Administration: Oral, 200 mg/kg, twice daily for 6 days
Result: Reduced Viremia and increased anti-FMD antibody titers, did not observe any clinical signs of FMD.
体内研究

T-1105 (Oral, 200 mg/kg, twice daily for 6 days) effectively inhibits the virus replication in the infected pigs[6].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pigs[6]
Dosage: 200 mg/kg
Administration: Oral, 200 mg/kg, twice daily for 6 days
Result: Reduced Viremia and increased anti-FMD antibody titers, did not observe any clinical signs of FMD.
性状Solid
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (179.71 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 7.1886 mL 35.9428 mL 71.8856 mL
5 mM 1.4377 mL 7.1886 mL 14.3771 mL
10 mM 0.7189 mL 3.5943 mL 7.1886 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (17.97 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (17.97 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (17.97 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (17.97 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

相关文档

化学品安全说明书(MSDS)

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风险声明 (欧洲) 36/37/38
安全声明 (欧洲) 26-37
海关编码 2934999090
Material Safety Data Sheet

Section1. Identification of the substance
3-Hydroxypyrazine-2-carboxamide
Product Name:
Synonyms:

Section2. Hazards identification
Harmful by inhalation, in contact with skin, and if swallowed.
H315:Causes skin irritation
H319:Causes serious eye irritation
H335:May cause respiratory irritation
P261:Avoid breathing dust/fume/gas/mist/vapours/spray
Wear protective gloves/protective clothing/eye protection/face protection
P280:
P305+P351+P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present
and easy to do – continue rinsing
P304+P340:IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing
P405:Store locked up

Section3. Composition/information on ingredients.
3-Hydroxypyrazine-2-carboxamide
Ingredient name:
CAS number:55321-99-8

Section4. First aid measures
Immediately wash skin with copious amounts of water for at least 15 minutes while removing
Skin contact:
contaminated clothing and shoes. If irritation persists, seek medical attention.
Eye contact:Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate
flushing of the eyes by separating the eyelids with fingers. If irritation persists, seek medical
attention.
Inhalation:Remove to fresh air. In severe cases or if symptoms persist, seek medical attention.
Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention.
Ingestion:

Section5. Fire fighting measures
In the event of a fire involving this material, alone or in combination with other materials, use dry
powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus
should be worn.

Section6. Accidental release measures
Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national
standards.
Respiratory precaution:Wear approved mask/respirator
Hand precaution:Wear suitable gloves/gauntlets
Skin protection:Wear suitable protective clothing
Eye protection:Wear suitable eye protection
Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container
for disposal. See section 12.
Environmental precautions: Do not allow material to enter drains or water courses.

Section7. Handling and storage
Handling:This product should be handled only by, or under the close supervision of, those properly qualified
in the handling and use of potentially hazardous chemicals, who should take into account the fire,
health and chemical hazard data given on this sheet.
Storage:Store in closed vessels.

Section8. Exposure Controls / Personal protection
Engineering Controls: Use only in a chemical fume hood.
Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles.
General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse.

Section9. Physical and chemical properties
Not specified
Appearance:
Boiling point:No data
Melting point:No data
Flash point:No data
Density:No data
Molecular formula:C5H5N3O2
Molecular weight:139.1

Section10. Stability and reactivity
Conditions to avoid: Heat, flames and sparks.
Materials to avoid: Oxidizing agents.
Possible hazardous combustion products: Carbon monoxide, nitrogen oxides.

Section11. Toxicological information
No data.

Section12. Ecological information
No data.

Section13. Disposal consideration
Arrange disposal as special waste, by licensed disposal company, in consultation with local waste
disposal authority, in accordance with national and regional regulations.

Section14. Transportation information
Non-harzardous for air and ground transportation.

Section15. Regulatory information
No chemicals in this material are subject to the reporting requirements of SARA Title III, Section
302, or have known CAS numbers that exceed the threshold reporting levels established by SARA
Title III, Section 313.


SECTION 16 - ADDITIONAL INFORMATION
N/A

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55321-99-8

文献:Pierra, Claire; Counor, Clement; Storer, Richard; Gosselin, Gilles Collection of Czechoslovak Chemical Communications, 2011 , vol. 76, # 11 p. 1327 - 1333

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55321-99-8结构式

55321-99-8

文献:Journal of the American Chemical Society, , vol. 69, p. 1034,1035 Journal of the American Chemical Society, , vol. 74, p. 3617,3618,3620

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55321-99-8结构式

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文献:Journal of the American Chemical Society, , vol. 69, p. 1034,1035

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55321-99-8结构式

55321-99-8

文献:Journal of Medicinal Chemistry, , vol. 26, # 2 p. 283 - 286

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