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

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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
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

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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

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

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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 75 India 1 United Kingdom 1 United States 10 Global 87

MedChemexpress LLC

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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

RQ-00203078, 10 mM in DMSO

1254205-52-1

C21H13ClF6N2O5S

Inhibitors