ChemicalBook > CAS DataBase List > RQ-00203078

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, 10 mM in DMSO;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
More
Less

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
InChI
InChI=1S/C21H13ClF6N2O5S/c22-17-9-14(20(23,24)25)10-29-18(17)30(11-12-1-5-15(6-2-12)35-21(26,27)28)36(33,34)16-7-3-13(4-8-16)19(31)32/h1-10H,11H2,(H,31,32)
InChIKey
IJGQFZYYEHCCIZ-UHFFFAOYSA-N
SMILES
C(O)(=O)C1=CC=C(S(N(C2=NC=C(C(F)(F)F)C=C2Cl)CC2=CC=C(OC(F)(F)F)C=C2)(=O)=O)C=C1
More
Less

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.

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1602
Product name
RQ-00203078
Purity
≥98% (HPLC)
Packaging
5 mg
Price
$154
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1602
Product name
RQ-00203078
Purity
≥98% (HPLC)
Packaging
25 mg
Price
$616
Updated
2025/07/31
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
More
Less

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

More
Less

RQ-00203078 Suppliers

China 75 India 1 United Kingdom 1 United States 10 Global 87
A.J Chemicals
Tel
--
Fax
--
Email
sales@ajchem.in
Country
India
ProdList
6100
Advantage
58
More
Less

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
  • RQ-00203078, 10 mM in DMSO
  • 1254205-52-1
  • C21H13ClF6N2O5S
  • Inhibitors