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433695-36-4生产厂家

433695-36-4价格

433695-36-4

433695-36-4结构式
433695-36-4结构式

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中文名 2-甲基-5-硝基-N,N-二甲基苯磺酰胺
英文名 N,N,2-trimethyl-5-nitrobenzenesulfonamide
中文别名 N,N,2-三甲基-5-硝基苯磺酰胺
英文别名 F1084-0159
Benzenesulfonamide,N,N,2-trimethyl-5-nitro
5-Nitro-2,N,N-trimethylbenzenesulfonamide
N,N,2-Trimethyl-5-nitrobenzenesulfonamide
BRL-50481
描述 BRL-50481 是 PDE7 的新型选择性抑制剂,对 PDE7A,PDE7B,PDE4 和 PDE3 的 IC50 值分别为 0.15,12.1,62 和 490 μM。
相关类别
靶点

IC50: 0.15 μM (PDE7A), 12 μM (PDE7B), 62 μM (PDE4), 490 μM (PDE3)[1]

体外研究 BRL-50481增加cAMP含量(300μM时IBMX响应的19.1±6.2%)但效果相当差。 BRL-50481(30μM)本身不能抑制增殖,但显着增强咯利普兰的作用。 BRL-50481(30μM)对IL-15诱导的增殖没有影响,但增强了咯利普兰的抑制作用。用BRL-50481预处理(30分钟)人单核细胞本身对所有测试浓度的TNFα输出具有可忽略的(~2-10%)抑制作用。 BRL-50481还增强PGE2对LPS诱导的TNFα释放的抑制作用。 BRL-50481本身对κB依赖性转录没有显着影响(在30μM时抑制率为5.6±1.9%)并且不能增强咯利普兰的作用(最大抑制,52.9±2.7%; pIC30值为5.33±0.12)。 BRL-50481以浓度依赖性方式抑制诱导PDE7A1的单核细胞中LPS诱导的TNFα释放(在12小时时间点30μM时抑制21.7±1.6%)[2]。
细胞实验 如图所示,用BRL-50481处理96孔板中的MOLT-4细胞30分钟。然后通过免疫特异性ELISA测定cAMP含量。结果表示为受100μMIBMX影响的响应百分比[2]。
参考文献

[1]. Safavi M, et al. New methods for the discovery and synthesis of PDE7 inhibitors as new drugs for neurologicaland inflammatory disorders. Expert Opin Drug Discov. 2013 Jun;8(6):733-51.

[2]. Smith SJ, et al. Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes. Mol Pharmacol. 2004 Dec;66(6):1679-89.

密度 1.334g/cm3
沸点 391.1ºC at 760 mmHg
熔点 73 °C
分子式 C9H12N2O4S
分子量 244.26800
闪点 190.4ºC
精确质量 244.05200
PSA 91.58000
LogP 2.75750
外观性状 固体;White to Light yellow powder to crystal
折射率 1.561
储存条件 0-10°C;避免加热

Section1. IDENTIFICATION OF THE SUBSTANCE/MIXTURE
Product identifiers
Product name: BRL 50481
CAS-No.: 433695-36-4
Relevant identified uses of the substance or mixture and uses advised against
Identified uses: Laboratory chemicals, Manufacture of substances



Section2. HAZARDS IDENTIFICATION
Classification of the substance or mixture
Not a hazardous substance or mixture according to Regulation (EC) No 1272/2008
This substance is not classified as dangerous according to Directive 67/548/EEC.
Label elements
Caution - substance not yet tested completely.
Other hazards - none

Section3. COMPOSITION/INFORMATION ON INGREDIENTS
Substances
Synonyms: 5-Nitro-2,N,N-trimethylbenzenesulfonamide
Formula: C9H12N2O4S C9H12N2O4S
Molecular Weight: 244,27 g/mol

Section4. FIRST AID MEASURES
Description of first aid measures
If inhaled
If breathed in, move person into fresh air. If not breathing, give artificial respiration.
In case of skin contact
Wash off with soap and plenty of water.
In case of eye contact
Flush eyes with water as a precaution.
If swallowed
Never give anything by mouth to an unconscious person. Rinse mouth with water.
Most important symptoms and effects, both acute and delayed
Indication of any immediate medical attention and special treatment needed
no data available

Section5. FIREFIGHTING MEASURES
Extinguishing media
Suitable extinguishing media
Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide.
Special hazards arising from the substance or mixture
Carbon oxides, nitrogen oxides (NOx), Sulphur oxides
Advice for firefighters
Wear self contained breathing apparatus for fire fighting if necessary.
Further information
no data available

Section6. ACCIDENTAL RELEASE MEASURES
Personal precautions, protective equipment and emergency procedures
Avoid dust formation. Avoid breathing vapors, mist or gas.
Environmental precautions
Do not let product enter drains.
Methods and materials for containment and cleaning up
Sweep up and shovel. Keep in suitable, closed containers for disposal.
Reference to other sections
For disposal see section 13.

Section7. HANDLING AND STORAGE
Precautions for safe handling
Provide appropriate exhaust ventilation at places where dust is formed.Normal measures for preventive fire
protection.
Conditions for safe storage, including any incompatibilities
Store in cool place. Keep container tightly closed in a dry and well-ventilated place.
Recommended storage temperature: 2 - 8 °C
Specific end uses
no data available

Section8. EXPOSURE CONTROLS/PERSONAL PROTECTION
Control parameters
Components with workplace control parameters
Exposure controls
Appropriate engineering controls
General industrial hygiene practice.
Personal protective equipment
Eye/face protection
Use equipment for eye protection tested and approved under appropriate government standards
such as NIOSH (US) or EN 166(EU).
Skin protection
Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique
(without touching glove's outer surface) to avoid skin contact with this product. Dispose of
contaminated gloves after use in accordance with applicable laws and good laboratory practices.
Wash and dry hands.
The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and
the standard EN 374 derived from it.
Body Protection
Choose body protection in relation to its type, to the concentration and amount of dangerous
substances, and to the specific work-place., The type of protective equipment must be selected
according to the concentration and amount of the dangerous substance at the specific workplace.
Respiratory protection
Respiratory protection is not required. Where protection from nuisance levels of dusts are desired,
use type N95 (US) or type P1 (EN 143) dust masks. Use respirators and components tested and
approved under appropriate government standards such as NIOSH (US) or CEN (EU).

Section9. PHYSICAL AND CHEMICAL PROPERTIES
Information on basic physical and chemical properties
a) AppearanceForm: solid
b) Odourno data available
c) Odour Thresholdno data available
d) pHno data available
e) Melting point/freezingno data available
point
f) Initial boiling point and no data available
boiling range
g) Flash pointno data available
h) Evaporation rateno data available
i) Flammability (solid, gas) no data available
j) Upper/lowerno data available
flammability or
explosive limits
k) Vapour pressureno data available
l) Vapour densityno data available
m) Relative densityno data available
n) Water solubilityno data available
o) Partition coefficient: n- log Pow: 0,436
octanol/water
p) Autoignitionno data available
temperature
q) Decompositionno data available
temperature
r) Viscosityno data available
s) Explosive propertiesno data available
t) Oxidizing propertiesno data available
Other safety information
no data available

Section10. STABILITY AND REACTIVITY
Reactivity
no data available
Chemical stability
no data available
Possibility of hazardous reactions
no data available
Conditions to avoid
no data available
Incompatible materials
Strong oxidizing agents
Hazardous decomposition products
Other decomposition products - no data available

Section11. TOXICOLOGICAL INFORMATION
Information on toxicological effects
Acute toxicity
no data available
Skin corrosion/irritation
no data available
Serious eye damage/eye irritation
no data available
Respiratory or skin sensitization
no data available
Germ cell mutagenicity
no data available
Carcinogenicity
IARC:No component of this product present at levels greater than or equal to 0.1% is identified as
probable, possible or confirmed human carcinogen by IARC.
Reproductive toxicity
no data available
Specific target organ toxicity - single exposure
no data available
Specific target organ toxicity - repeated exposure
no data available
Aspiration hazard
no data available
Potential health effects
Inhalation
May be harmful if inhaled. May cause respiratory tract irritation.
IngestionMay be harmful if swallowed.
SkinMay be harmful if absorbed through skin. May cause skin irritation.
EyesMay cause eye irritation.
Additional Information
RTECS: Not available

Section12. ECOLOGICAL INFORMATION
Toxicity
no data available
Persistence and degradability
no data available
Bioaccumulative potential
no data available
Mobility in soil
no data available
Results of PBT and vPvB assessment
no data available
Other adverse effects
no data available

Section13. DISPOSAL CONSIDERATIONS
Waste treatment methods
Product
Offer surplus and non-recyclable solutions to a licensed disposal company.
Contaminated packaging
Dispose of as unused product.

Section14. TRANSPORT INFORMATION
UN number
ADR/RID: -IMDG: -IATA: -
UN proper shipping name
ADR/RID: Not dangerous goods
IMDG: Not dangerous goods
IATA:Not dangerous goods
Transport hazard class(es)
ADR/RID: -IMDG: -IATA: -
Packaging group
ADR/RID: -IMDG: -IATA: -
Environmental hazards
ADR/RID: noIMDG Marine pollutant: noIATA: no
Special precautions for user
no data available

Section15. REGULATORY INFORMATION
This safety datasheet complies with the requirements of Regulation (EC) No. 1907/2006.
Safety, health and environmental regulations/legislation specific for the substance or mixture
no data available
Chemical Safety Assessment
no data available

Section16. OTHER INFORMATION
Further information
Copyright 2012 Co. LLC. License granted to make unlimited paper copies for internal use
only.
The above information is believed to be correct but does not purport to be all inclusive and shall be
used only as a guide. The information in this document is based on the present state of our knowledge
and is applicable to the product with regard to appropriate safety precautions. It does not represent any
guarantee of the properties of the product. Corporation and its Affiliates shall not be held
liable for any damage resulting from handling or from contact with the above product. See
and/or the reverse side of invoice or packing slip for additional terms and conditions of sale.
个人防护装备 Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
危险品运输编码 NONH for all modes of transport