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RQ-00203078

Product Name
RQ-00203078
CAS No.
1254205-52-1
Chemical Name
RQ-00203078
Synonyms
CS-1528;RQ-00203078;RQ-00203078 >=98% (HPLC);RQ-00203078;RQ 00203078;RQ00203078.;4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid;4-{[3-chloro-5-(trifluoromethyl)pyridin-2-yl]({[4-(trifluoromethoxy)phenyl]methyl})sulfamoyl}benzoic acid;4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid;Benzoic acid, 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-;Transient receptor potential channels,Ca2+,TRPM8,RQ00203078,TRP Channel,migration,inhibit,Inhibitor,RQ 00203078,RQ-00203078,oral,invasion,menthol
CBNumber
CB93040792
Molecular Formula
C21H13ClF6N2O5S
Formula Weight
554.85
MOL File
1254205-52-1.mol
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RQ-00203078 Property

Boiling point:
602.0±65.0 °C(Predicted)
Density 
1.588±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥27.25 mg/mL in EtOH
form 
solid
pka
3.39±0.10(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
19075
Product name
RQ-00203078
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
19075
Product name
RQ-00203078
Purity
≥98%
Packaging
5mg
Price
$122
Updated
2024/03/01
Cayman Chemical
Product number
19075
Product name
RQ-00203078
Purity
≥98%
Packaging
10mg
Price
$199
Updated
2024/03/01
Tocris
Product number
5388
Product name
RQ00203078
Purity
≥98%(HPLC)
Packaging
10
Price
$208
Updated
2021/12/16
Tocris
Product number
5388
Product name
RQ00203078
Purity
≥98%(HPLC)
Packaging
50
Price
$870
Updated
2021/12/16
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RQ-00203078 Chemical Properties,Usage,Production

Description

RQ-00203078 is a selective antagonist of transient receptor potential melastatin 8 (TRPM8; IC50s = 8.3 and 5.8 nM in human and rat, respectively), while having little inhibitory action against TRPV1 (IC50 > 30 μM), TRPA1 (IC50 > 10 μM), TRPV4 (IC50 = 10 μM), or TRPM2 channels (IC50 > 10 μM). It attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg) after oral administration. RQ-00203078 has been shown to reduce HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro. TRPM8, a member of the TRP melastatin subgroup, plays a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy, diabetic neuropathy, migraine, and overactive bladder. It is also known to be involved in the tumor progression of certain carcinomas.

Uses

RQ 00203078 is a selective and orally active TRPM8 antagonist.

in vitro

in the menthol-induced calcium influx assay, rq-00203078 is a novel and highly potent trpm8 antagonist with human and rat ic50 values of 8.3 nm and 5.8 nm, respectively. rq-00203078 was highly selective over other trp channels [1].

in vivo

rq-00203078 demonstrated excellent activity in vivo in a dose dependent manner with an ed50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration [1].

IC 50

8.3 and 5.8 nm for htrpm8 and rtrpm8, respectively

storage

Store at +4°C

References

[1] ohmi m, shishido y, inoue t, ando k, fujiuchi a, yamada a, watanabe s, kawamura k. identification of a novel 2-pyridyl-benzensulfonamide derivative, rq-00203078, as a selective and orally active trpm8 antagonist. bioorg med chem lett. 2014 dec 1;24(23):5364-8.

RQ-00203078 Preparation Products And Raw materials

Raw materials

Preparation Products

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RQ-00203078 Suppliers

China 60 India 1 United Kingdom 1 United States 10 Global 72
Tocris Bioscience
Tel
--
Fax
--
Email
customerservice@tocris.co.uk
Country
United Kingdom
ProdList
5726
Advantage
77
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View Lastest Price from RQ-00203078 manufacturers

Career Henan Chemical Co
Product
RQ-00203078 1254205-52-1
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2019-12-30
Career Henan Chemical Co
Product
RQ-00203078 1254205-52-1
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2019-12-30

1254205-52-1, RQ-00203078Related Search:


  • RQ-00203078;RQ 00203078;RQ00203078.
  • CS-1528
  • 4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid
  • RQ-00203078
  • 4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid
  • Benzoic acid, 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-
  • RQ-00203078 >=98% (HPLC)
  • Transient receptor potential channels,Ca2+,TRPM8,RQ00203078,TRP Channel,migration,inhibit,Inhibitor,RQ 00203078,RQ-00203078,oral,invasion,menthol
  • 4-{[3-chloro-5-(trifluoromethyl)pyridin-2-yl]({[4-(trifluoromethoxy)phenyl]methyl})sulfamoyl}benzoic acid
  • 1254205-52-1
  • C21H13ClF6N2O5S
  • Inhibitors