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
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
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.
N-Bromosuccinimide Price
- Product number
- 19075
- Product name
- RQ-00203078
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 19075
- Product name
- RQ-00203078
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $122
- Updated
- 2024/03/01
- Product number
- 19075
- Product name
- RQ-00203078
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $199
- Updated
- 2024/03/01
- Product number
- 5388
- Product name
- RQ00203078
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $208
- Updated
- 2021/12/16
- Product number
- 5388
- Product name
- RQ00203078
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $870
- Updated
- 2021/12/16
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-
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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View Lastest Price from RQ-00203078 manufacturers
- 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
- 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