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
- Molecular Weight:
- 554.85
- MDL Number:
- MFCD29049510
- MOL File:
- 1254205-52-1.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| 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 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) | ![]() GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| target organs | Respiratory system | |||||||||
| WGK Germany | WGK 3 | |||||||||
| Storage Class | 11 - Combustible Solids | |||||||||
| Hazard Classifications | Eye Irrit. 2 Skin Irrit. 2 STOT SE 3 |
|||||||||
| NFPA 704 |
|
RQ-00203078 price More Price(43)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1602 | RQ-00203078 ≥98% (HPLC) | 1254205-52-1 | 5 mg | $165 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML1602 | RQ-00203078 ≥98% (HPLC) | 1254205-52-1 | 25 mg | $660 | 2026-04-30 | Buy |
| Cayman Chemical | 19075 | RQ-00203078 ≥98% | 1254205-52-1 | 1mg | $36 | 2026-04-30 | Buy |
| Cayman Chemical | 19075 | RQ-00203078 ≥98% | 1254205-52-1 | 5mg | $135 | 2026-04-30 | Buy |
| Cayman Chemical | 19075 | RQ-00203078 ≥98% | 1254205-52-1 | 10mg | $219 | 2026-04-30 | Buy |
RQ-00203078 Chemical Properties, Uses, 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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2915 | 55 | |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7545 | 61 |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4853 | 58 |
| Bide Pharmatech Ltd. | 400-164-7117 18317119277 | product02@bidepharm.com | China | 40000 | 60 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4859 | 55 | |
| Shanghaizehan biopharma technology co., Ltd. | 021-61350663 13052117465 | sales@zehanbiopharma.com | China | 989 | 55 |
| Guangzhou Zhiya Chemdrugs Co.,Ltd | 18122150900 | sculk28@163.com | China | 645 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Guangzhou QiYun Biotechnology Co., Ltd. | 020-61288194 61288195 | 505721671@qq.com | China | 3853 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
View Latest Price from RQ-00203078 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
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2026-07-17 | RQ-00203078
1254205-52-1
|
$43.00-126.00 | 99.60% | 10g | TargetMol Chemicals Inc. | ||
![]() |
2019-12-31 | RQ-00203078
1254205-52-1
|
$1.00 | 1KG | Min98% HPLC | Career Henan Chemical Co | ||
![]() |
2019-12-31 | RQ-00203078
1254205-52-1
|
$1.00 | 1KG | Min98% HPLC | Career Henan Chemical Co |
-

- RQ-00203078
1254205-52-1
- $43.00-126.00
- 99.60%
- TargetMol Chemicals Inc.
-

- RQ-00203078
1254205-52-1
- $1.00
- Min98% HPLC
- Career Henan Chemical Co
-

- RQ-00203078
1254205-52-1
- $1.00
- Min98% HPLC
- Career Henan Chemical Co





